[{"id":"i131-mibg","kind":"drug","name":"131I-MIBG (iobenguane I-131) therapy","aka":[],"tldr":"High-dose radioactive MIBG delivers radiation from inside neuroblastoma cells that take up noradrenaline; used for relapsed disease and tested in upfront therapy.","summary":"Response rate ~30-40% in relapsed/refractory MIBG-avid neuroblastoma (NANT, COG studies), with myelosuppression requiring stem-cell support at ≥12 mCi/kg. COG ANBL1531 randomised 131I-MIBG added to induction (primary results pending 2026). Commercial Azedra (for pheochromocytoma) was discontinued in 2024, leaving compounding and academic supply.","status":"established","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Iobenguane","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Iobenguane"}],"tags":[],"related":["i-131"],"indications":["neuroblastoma","neuroblastoma-high-risk","metastatic-ppgl"],"sections":[],"technologies":["mibg-theranostics","radioligand-therapy"],"targets":[],"drugs":[],"companies":["lantheus"],"institutions":[],"pathways":[],"terms":[],"trials":["anbl1531"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"Radioligand therapy (beta, norepinephrine transporter)","mechanism":"Norepinephrine transporter uptake of radio-iodinated benzylguanidine; 131I beta emission (2 mm range).","approvals":[],"mechanismSteps":[],"dosing":{"route":"IV","schedule":"12-18 mCi/kg single or tandem doses with autologous stem-cell support; thyroid blockade with potassium iodide","monitoring":"Radiation isolation, counts, thyroid function, secondary malignancy"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"itm-11","kind":"drug","name":"177Lu-edotreotide","aka":[],"tldr":"A second lutetium radioligand for neuroendocrine tumours that beat the standard pill everolimus in a head-to-head trial and is awaiting an FDA decision.","summary":"COMPETE (Lancet 2025; 309 patients, grade 1-2 GEP-NETs): PFS 23.9 vs 14.1 months versus everolimus (HR 0.67); response rate higher; interim OS 63.4 vs 58.7 months, a difference that did not reach statistical significance (HR 0.78). Uses non-carrier-added 177Lu from ITM's own supply. NDA accepted with PDUFA 28 August 2026. COMPOSE (grade 2-3, versus CAPTEM/everolimus/FOLFOX) ongoing.","status":"phase-3","asOf":"2026-09-07","links":[{"label":"ClinicalTrials.gov NCT03049189 (COMPETE)","url":"https://clinicaltrials.gov/study/NCT03049189"}],"tags":[],"related":["lu-177"],"indications":["neuroendocrine","grade-3-net"],"sections":[],"technologies":["prrt","radioligand-therapy"],"targets":["sstr2"],"drugs":[],"companies":["itm"],"institutions":[],"pathways":[],"terms":[],"trials":["compete","nct04919226"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"ITM-11, n.c.a. 177Lu-DOTATOC","modality":"Radioligand therapy (beta)","mechanism":"DOTATOC peptide (SSTR2 agonist) chelating 177Lu; four cycles of 7.5 GBq every 3 months.","approvals":[],"mechanismSteps":[],"dosing":{"route":"Intravenous","schedule":"7.5 GBq every 3 months × 4 with amino-acid renal protection"},"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2025-03","type":"designation","region":"US","note":"COMPETE topline at ENETS 2025","source":"https://www.itm-radiopharma.com/news/press-releases/press-releases-detail/itm-presents-positive-topline-phase-3-compete-trial-data-with-nca-177lu-edotreotide-itm-11-a-targeted-radiopharmaceutical-therapy-in-patients-with-grade-1-or-2-gastroenteropancreatic-neuroendocrine-tumors-at-the-enets-2025-conference-688/"},{"date":"2026-08-28","type":"pdufa","region":"US","note":"PDUFA goal date for GEP-NET indication","source":"https://www.cancernetwork.com/view/fda-accepts-new-drug-application-for-177lu-edotreotide-in-gep-nets"}]},{"id":"lu177-psma-it","kind":"drug","name":"177Lu-PSMA-I&T","aka":[],"tldr":"177Lu-PSMA-I&T is a second PSMA radioligand, chemically different from Pluvicto, that has passed two phase 3 trials on progression but has not yet shown a survival benefit.","summary":"SPLASH (Lantheus PNT2002, ESMO 2024): rPFS 9.5 vs 6.0 months (HR 0.71) vs ARPI switch in taxane-naive mCRPC; interim OS HR 1.11 (immature, crossover). ECLIPSE (Curium, 7.4 GBq × 6): met rPFS endpoint vs ARPI in the same setting; OS maturing; FDA submission plan pending. Curium's Japanese registrational trial with PeptiDream started February 2026. Widely used off-protocol in Germany and Australia.","status":"phase-3","asOf":"2026-09-06","links":[{"label":"SPLASH primary analysis (Lantheus, ESMO 2024)","url":"https://lantheusholdings.gcs-web.com/news-releases/news-release-details/lantheus-presents-results-primary-analysis-phase-3-pivotal"},{"label":"ECLIPSE meets rPFS (OncLive)","url":"https://www.onclive.com/view/177lu-psma-i-t-meets-rpfs-end-point-in-psma-mcrpc"}],"tags":[],"related":["lu-177"],"indications":["prostate","prostate-mcrpc"],"sections":[],"technologies":["radioligand-therapy","psma-pet"],"targets":["psma"],"drugs":[],"companies":["lantheus","curium"],"institutions":[],"pathways":[],"terms":[],"trials":["splash","eclipse-psma"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"PNT2002 (Lantheus); Curium 177Lu-PSMA-I&T","modality":"Radioligand therapy (beta)","mechanism":"Urea-based PSMA ligand with DOTAGA chelator carrying 177Lu; beta emission.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"alphamedix","kind":"drug","name":"212Pb-DOTAMTATE","aka":[],"tldr":"An alpha-particle version of neuroendocrine radioligand therapy that produced responses in over half of patients who had never had PRRT, with FDA Breakthrough designation.","summary":"ALPHAMEDIX-02 (Sanofi/Orano Med/RadioMedix, October 2025): met all primary endpoints; ORR 54.3% in PRRT-naive patients with ~70-75% progression-free at about 3 years, and durable disease control in PRRT-exposed patients (~83% progression-free at 18 months). Breakthrough Therapy designation 2024. Sanofi acquired global rights (2024); registrational strategy under discussion. Supply relies on Orano Med's 212Pb generators.","status":"phase-2","asOf":"2026-09-07","links":[{"label":"Sanofi press release Oct 2025","url":"https://www.sanofi.com/en/media-room/press-releases/2025/2025-10-08-05-00-00-3163053"}],"tags":[],"related":["pb-212"],"indications":["neuroendocrine"],"sections":[],"technologies":["prrt","targeted-alpha-therapy"],"targets":["sstr2"],"drugs":[],"companies":["orano-med","radiomedix"],"institutions":[],"pathways":[],"terms":[],"trials":["alphamedix-02"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"AlphaMedix","modality":"Targeted alpha therapy (lead-212)","mechanism":"DOTAMTATE (SSTR2 agonist) chelating 212Pb, which decays via 212Bi to emit an alpha particle at the tumour cell.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"aaa817","kind":"drug","name":"AAA817","aka":["[225Ac]Ac-PSMA-617"],"tldr":"AAA817 is an experimental radioligand therapy from Novartis Pharmaceuticals in phase 3 trials for prostate cancer, aimed at PSMA.","summary":"AAA817 is a radioligand therapy developed by Novartis Pharmaceuticals. Its target is PSMA (the sponsor names PSMA). The sponsor states: Inside the body, AAA817 ([225Ac]Ac-PSMA-617) attaches to PSMA on the surface of prostate cancer cells and emits radiation to kill them; this treatment is also called a radioligand therapy. ClinicalTrials.gov describes the intervention as: AAA817 is being studied for treating PSMA positive mCRPC. Inside the body, it attaches itself to PSMA on the cell surface of the prostate cancer cells and emits radiation to kill them. This treatment is also called a radioligand therapy. It is the investigational product in 2 recruiting or active industry-led phase 2 and phase 3 interventional cancer trials, including phase 3 studies NCT06855277 (Study Comparing AAA817+ARPI Versus Standard of Care in Adult Participants With PSMA-positive mCRPC) and NCT06780670 (Open-label Study Comparing AAA817 Versus Standard of Care in the Treatment of Previously Treated PSMA-positive mCRPC Adults Who Have Disease Progressed on or After [177Lu]Lu-PSMA Targeted Therapy), in prostate cancer. The largest, NCT06855277, plans to enrol 940 participants with primary completion expected 2028-09-29. Status reflects the highest phase registered on ClinicalTrials.gov; no efficacy results are recorded here.","status":"phase-3","asOf":"2026-09-11","links":[{"label":"ClinicalTrials.gov: trials of AAA817","url":"https://clinicaltrials.gov/search?intr=AAA817"}],"tags":["pipeline","ctgov-ingest"],"related":["lu-177","ac-225"],"indications":["prostate"],"sections":[],"technologies":[],"targets":["psma"],"drugs":[],"companies":["novartis"],"institutions":[],"pathways":[],"terms":[],"trials":["nct06855277","nct06780670"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2 + sponsor pipeline pages)","editedOn":"2026-09-11"},"modality":"radioligand","mechanism":"Inside the body, AAA817 ([225Ac]Ac-PSMA-617) attaches to PSMA on the surface of prostate cancer cells and emits radiation to kill them; this treatment is also called a radioligand therapy.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"abiraterone","kind":"drug","name":"Abiraterone acetate","aka":[],"tldr":"Abiraterone is a pill that shuts down testosterone production everywhere, including inside the tumour. Discovered at the Institute of Cancer Research, now generic and used from the first metastatic diagnosis.","summary":"Abiraterone acetate irreversibly inhibits CYP17A1 (17-alpha-hydroxylase and 17,20-lyase), shutting down androgen synthesis in the adrenal glands and inside the tumour, not just the testes; it is given with prednisone to offset mineralocorticoid excess. Its evidence spans advanced prostate cancer: COU-AA-301 and 302 (mCRPC post- and pre-docetaxel), LATITUDE and STAMPEDE (mHSPC, overall survival benefit; LATITUDE OS 53.3 versus 36.5 months, HR 0.66) and PEACE-1 (triplet with docetaxel). Generic since 2018 to 2019, it is the backbone partner for PARP inhibitors (PROpel, MAGNITUDE), capivasertib (CAPItello-281) and Pluvicto (PSMAddition). Open questions are how to choose between abiraterone and the AR antagonists, and which men need a third drug. Discovered at the Institute of Cancer Research, it is the affordable hormone pill most men with metastatic prostate cancer now start at diagnosis.","status":"approved","asOf":"2026-09-06","wikipedia":"https://en.wikipedia.org/wiki/Abiraterone_acetate","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Abiraterone%20acetate"}],"tags":[],"related":[],"indications":["prostate","prostate-mhspc","prostate-mcrpc","prostate-high-risk"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["johnson-johnson"],"institutions":["royal-marsden"],"pathways":[],"terms":[],"trials":["stampede","nct06520345","nct07611110"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Zytiga (generic)","modality":"Small-molecule CYP17A1 inhibitor","mechanism":"Irreversible CYP17A1 (17α-hydroxylase/17,20-lyase) inhibition blocks adrenal and intratumoural androgen synthesis.","approvals":[{"region":"US","year":2011,"indication":"mCRPC after docetaxel"},{"region":"US","year":2012,"indication":"mCRPC pre-chemotherapy"},{"region":"US","year":2018,"indication":"High-risk mHSPC (LATITUDE)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ryz101","kind":"drug","name":"Actinium-225 DOTATATE","aka":[],"tldr":"An alpha-particle version of Lutathera for neuroendocrine tumours that have stopped responding to the beta version.","summary":"RYZ101 is actinium-225 DOTATATE, a targeted alpha therapy: the same SSTR2-binding peptide as Lutathera but chelating 225Ac, whose alpha decay chain delivers dense, short-range double-strand DNA breaks that beta particles cannot match. Bristol Myers Squibb acquired it with RayzeBio in 2024 for $4.1B. The ACTION-1 phase 3 trial tests it in SSTR-positive GEP-NETs progressing after 177Lu-SSTR therapy, at 10.5 MBq/kg every 8 weeks for 4 cycles, and it is also being combined with chemo-immunotherapy in extensive-stage small-cell lung cancer. Nausea, fatigue and lymphopenia are expected, and renal function is monitored because the kidneys clear the peptide. Whether alpha emission overcomes resistance to beta therapy, and whether 225Ac supply can meet demand, are the open questions. For a newcomer: an alpha-particle upgrade of an approved neuroendocrine radioligand.","status":"phase-3","asOf":"2026-09-04","links":[{"label":"ClinicalTrials.gov: trials of Actinium-225 DOTATATE","url":"https://clinicaltrials.gov/search?intr=RYZ101"}],"tags":[],"related":["lu-177","ac-225"],"indications":["neuroendocrine","sclc"],"sections":[],"technologies":["targeted-alpha-therapy"],"targets":["sstr2"],"drugs":[],"companies":["bms","rayzebio"],"institutions":[],"pathways":[],"terms":[],"trials":["nct06590857"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"RYZ101","modality":"Targeted alpha therapy","mechanism":"DOTATATE chelating 225Ac; alpha decay chain.","approvals":[],"mechanismSteps":["Radioligand circulates and binds Somatostatin receptor 2 on tumour cells","Ligand is internalised or retained at the membrane","Alpha (225Ac) emissions deposit energy within a short range","Clustered DNA double-strand breaks form in the tumour cell and its neighbours (crossfire)","Cells die; unbound ligand is cleared via the kidneys"],"dosing":{"route":"IV infusion","schedule":"10.5 MBq/kg every 8 weeks for 4 cycles (ACTION-1)","monitoring":"Renal function, blood counts, amino acid co-infusion","source":"https://clinicaltrials.gov/study/NCT05477576"},"toxicity":[{"event":"Nausea"},{"event":"Fatigue"},{"event":"Lymphopenia"},{"event":"Renal toxicity (monitor)"}],"access":[{"country":"US","reimbursement":"Investigational","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2024-02-26","type":"filing","region":"US","note":"BMS completes RayzeBio acquisition ($4.1B)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},{"id":"ac-225-fpi-2068","kind":"drug","name":"Actinium-225 FPI-2068","aka":["225Ac-FPI-2068","[225Ac]-FPI-2068"],"tldr":"An antibody engineered to grab onto two markers found together on some solid tumours, but not on healthy cells, carries a powerful short-range radioactive payload into the tumour to try to destroy it.","summary":"225Ac-FPI-2068 is a bispecific targeted alpha therapy (TAT) from Fusion Pharmaceuticals, developed jointly with AstraZeneca, designed for solid tumours that co-express EGFR and cMET (including head and neck squamous cell carcinoma, non-small cell lung cancer, colorectal cancer and pancreatic ductal adenocarcinoma). It combines the bispecific antibody FPI-2053 with the alpha emitter actinium-225 via a DOTA chelate; an indium-111-labelled version of the same antibody (FPI-2107) is used as a companion imaging and dosimetry tracer, and unlabelled FPI-2053 is given as a pre-dose to optimise biodistribution.\n\nPreclinical data presented at AACR-NCI-EORTC in 2023 showed FPI-2068 bound EGFR/cMET-expressing colorectal and lung cancer cell lines, internalised into tumour cells, and caused prolonged tumour regression (over 28 days) in xenograft models at doses of 370-740 kBq/kg, with evidence of DNA double-strand break formation and apoptosis consistent with its proposed mechanism. The FDA cleared investigational new drug (IND) applications for FPI-2068 and FPI-2107 in April 2023.\n\nA first-in-human phase 1, two-part, dose-escalation trial (ClinicalTrials.gov NCT06147037) opened in July 2024 across US and Canadian sites, evaluating safety, tolerability, dosimetry, biodistribution and pharmacokinetics in adults with advanced EGFR/cMET-co-expressing solid tumours; Part A optimises the FPI-2053 pre-dose and Part B escalates the actinium-225 dose. As of the most recent public update (October 2025), no human efficacy or safety results had been reported; the study's estimated primary completion is December 2026/2027.","status":"phase-1","asOf":"2026-09-22","links":[{"label":"Fusion Pharmaceuticals: AACR-NCI-EORTC 2023 preclinical poster on FPI-2068","url":"https://fusionpharma.com/wp-content/uploads/2023/10/2068_AACR-poster_2023_Final.pdf"},{"label":"Fusion Pharmaceuticals: IND clearance for FPI-2068 and FPI-2107, April 2023","url":"https://www.pharmaceutical-technology.com/news/fusion-fda-ind-fpi-2068/"},{"label":"ClinicalTrials.gov: NCT06147037","url":"https://clinicaltrials.gov/study/NCT06147037"}],"tags":["alpha therapy","bispecific antibody","EGFR","cMET","actinium-225","phase 1"],"related":["fpi-2265","in-111","ac-225"],"indications":[],"sections":[],"technologies":["targeted-alpha-therapy"],"targets":[],"drugs":[],"companies":["fusion-pharma","astrazeneca"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["EGFR and cMET are not yet represented as target records in this graph, so no targets[] link is made here; add them once those target records exist."],"code":"FPI-2068","modality":"alpha therapy","mechanism":"A bispecific, humanised IgG antibody (FPI-2053) that binds both EGFR and cMET, conjugated via a DOTA chelator to the alpha-emitting radioisotope actinium-225. Because it targets two receptors that are co-expressed on tumour cells but not usually together on normal tissue, the antibody is designed to internalise preferentially into tumour cells, delivering alpha particles that cause DNA double-strand breaks.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ac225-psma","kind":"drug","name":"Actinium-225 PSMA agents","aka":[],"tldr":"Alpha-emitting PSMA drugs that produce responses even after Pluvicto fails, held back mainly by isotope supply.","summary":"Novartis (225Ac-PSMA-617, phase 3 AcTION), Bayer (225Ac-PSMA-Trillium with albumin binder, PAnTHA phase 1 at ASCO GU 2026), Fusion/AstraZeneca (FPI-2265, 225Ac-PSMA-I&T, phase 3 AlphaBreak), and academic 225Ac-PSMA data from South Africa and Germany. Xerostomia from salivary uptake is dose-limiting.","status":"phase-3","asOf":"2026-09-04","links":[{"label":"ClinicalTrials.gov: trials of Actinium-225 PSMA agents","url":"https://clinicaltrials.gov/search?intr=225Ac-PSMA-617"}],"tags":[],"related":["ac-225"],"indications":["prostate","prostate-mcrpc"],"sections":[],"technologies":["targeted-alpha-therapy"],"targets":["psma"],"drugs":[],"companies":["novartis","bayer","fusion-pharma","astrazeneca"],"institutions":[],"pathways":[],"terms":[],"trials":["nct07590934"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"225Ac-PSMA-617, 225Ac-PSMA-I&T, BAY 3563254 (Trillium)","modality":"Targeted alpha therapy","mechanism":"PSMA ligand with 225Ac; four alpha emissions per decay chain.","approvals":[],"mechanismSteps":["Radioligand circulates and binds PSMA on tumour cells","Ligand is internalised or retained at the membrane","Alpha (225Ac) emissions deposit energy within a short range","Clustered DNA double-strand breaks form in the tumour cell and its neighbours (crossfire)","Cells die; unbound ligand is cleared via the kidneys"],"dosing":{"route":"IV infusion","schedule":"Trial regimens ~100 kBq/kg every 6-8 weeks","monitoring":"Salivary gland toxicity (xerostomia), renal function, blood counts","source":"https://clinicaltrials.gov"},"toxicity":[{"event":"Xerostomia","note":"Dose-limiting in academic series"},{"event":"Anaemia"},{"event":"Thrombocytopenia"},{"event":"Renal toxicity"}],"access":[{"country":"US","reimbursement":"Investigational (phase 3)","asOf":"2026-09-06"},{"country":"DE","reimbursement":"Compassionate use at selected centres (Heidelberg and others)","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2024-06","type":"filing","region":"US","note":"AstraZeneca completes Fusion Pharmaceuticals acquisition; FPI-2265 phase 3 planned","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},{"id":"al2846","kind":"drug","name":"AL2846","aka":[],"tldr":"AL2846 is an experimental small-molecule drug from Chia Tai Tianqing Pharmaceutical in phase 3 trials for thyroid cancer, aimed at MET and RET.","summary":"AL2846 is a small-molecule drug developed by Chia Tai Tianqing Pharmaceutical. Its targets are MET, RET and KIT (the sponsor names c-MET, c-KIT, VEGFR1, RET). The sponsor states: A multi-target tyrosine kinase inhibitor capsule with significant inhibitory effects on c-MET, c-KIT, VEGFR1 and RET. ClinicalTrials.gov describes the intervention as: AL2846 Capsule is a multi - target tyrosine kinase inhibitor, which has significant inhibitory effects on c-Mesenchymal-epithelial transition factor (c - MET), stem cell factor receptor (c - KIT), VEGFR1 and Ret Proto-Oncogene (RET). It is the investigational product in 1 recruiting or active industry-led phase 2 and phase 3 interventional cancer trial, including the phase 3 study NCT06860971 (A Study of AL2846 Capsule Versus Placebo in the Treatment of Advanced Radioiodine-Refractory Differentiated Thyroid Carcinoma), in thyroid cancer. The largest, NCT06860971, plans to enrol 144 participants with primary completion expected 2027-01. Status reflects the highest phase registered on ClinicalTrials.gov; no efficacy results are recorded here.","status":"phase-3","asOf":"2026-09-11","links":[{"label":"ClinicalTrials.gov: trials of AL2846","url":"https://clinicaltrials.gov/search?intr=AL2846"}],"tags":["pipeline","ctgov-ingest"],"related":[],"indications":["thyroid"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["nct06860971"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2 + sponsor pipeline pages)","editedOn":"2026-09-11"},"modality":"small molecule (structure undisclosed or not yet in PubChem)","mechanism":"A multi-target tyrosine kinase inhibitor capsule with significant inhibitory effects on c-MET, c-KIT, VEGFR1 and RET.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"n-13-ammonia","kind":"drug","name":"Ammonia N-13","aka":["13N-ammonia","N-13 ammonia"],"tldr":"A radioactive form of ammonia gas, made fresh on site in a cyclotron and injected into a vein; heart muscle cells trap it in proportion to how much blood is flowing through, so a PET scan maps blood flow to the heart very precisely.","summary":"Ammonia N-13 injection is a cyclotron-produced PET myocardial perfusion agent, initial US approval 2007 (NDA 22-119, full approval 2011), taken up and metabolically trapped in myocytes as N-13 glutamine, giving image quality and quantitative accuracy that ASNC/SNMMI guidelines rate among the best of the FDA-approved and CMS-reimbursable PET perfusion tracers (the others being Rb-82; O-15 water is used in Europe but is not FDA approved).\n\nThe FDA label indicates it for diagnostic PET imaging of the myocardium under rest or pharmacologic stress to evaluate myocardial perfusion in patients with suspected or existing coronary artery disease. The recommended adult dose is 10-20 mCi (0.368-0.736 GBq) as an intravenous bolus for each of the rest and stress studies, with the stress study begun 40 minutes or more after the first injection to allow adequate decay of the 9.97-minute isotope; imaging starts about 3 minutes after injection.\n\nBecause it requires an on-site or very nearby cyclotron (unlike generator-based Rb-82), N-13 ammonia's use is concentrated at academic and large hospital PET centres; it is the other guideline-endorsed option, alongside Rb-82, for the resting perfusion half of the two-part cardiac sarcoidosis PET protocol, and is favoured by some centres for absolute myocardial blood flow quantification given its longer half-life relative to Rb-82, which allows more complete kinetic sampling.","asOf":"2026-09-22","links":[{"label":"FDA label: Ammonia N 13 Injection, 2011 revision","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022119s001lbl.pdf"},{"label":"FDA approval package, NDA 22-119/S-001","url":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022119orig1s001.pdf"},{"label":"ASNC/SNMMI PET nuclear cardiology procedure standard","url":"https://www.asnc.org/wp-content/uploads/2024/06/s12350-016-0522-3.pdf"}],"tags":["PET","myocardial perfusion","cyclotron"],"related":["rb-82-chloride","f-18-flurpiridaz","n-13","o-15","rb-82"],"indications":["coronary-artery-disease","cardiac-sarcoidosis"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"N-13 ammonia (as NH3/NH4+) diffuses into myocytes and is metabolically trapped as N-13 glutamine by glutamine synthetase, giving high myocardial uptake proportional to blood flow. Its 9.97-minute physical half-life requires an on-site cyclotron, in contrast to generator-produced Rb-82, but permits standard two- or three-compartment kinetic modelling for absolute myocardial blood flow quantification (mL/min/g) using dynamic PET acquisition.","approvals":[{"region":"US","year":2007,"indication":"Diagnostic PET imaging of the myocardium under rest or pharmacologic stress to evaluate myocardial perfusion in patients with suspected or existing coronary artery disease"}],"mechanismSteps":[],"dosing":{"route":"Intravenous bolus injection","schedule":"10-20 mCi (0.368-0.736 GBq) per rest or stress study; imaging begins about 3 minutes after injection for 10-20 minutes; stress study begun 40+ minutes after the rest dose","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022119s001lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"cabazitaxel","kind":"drug","name":"Cabazitaxel","aka":[],"tldr":"A second taxane that works after docetaxel and beat a second hormone pill head-to-head (CARD).","summary":"Cabazitaxel is a taxane with low affinity for the P-glycoprotein efflux pump, so it remains active in docetaxel-resistant disease. It is used in metastatic castration-resistant prostate cancer after docetaxel, with neutropenia as its main toxicity. TROPIC (2010) showed an overall survival benefit after docetaxel, and CARD (2019) showed it was superior to switching to a second androgen receptor pathway inhibitor in men who had already had one ARPI and docetaxel. It served as the comparator in TheraP, where it lost to 177Lu-PSMA-617 on PSA50 response (66% versus 37%) although overall survival was similar (HR 0.97), and in XALute against the T-cell engager xaluritamig. Its place relative to radioligands and T-cell engagers is therefore still being worked out. For a newcomer, it is the second taxane that works after docetaxel and beat a second hormone pill head-to-head.","status":"approved","asOf":"2026-09-06","wikipedia":"https://en.wikipedia.org/wiki/Cabazitaxel","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Cabazitaxel"}],"tags":[],"related":["lu-177"],"indications":["prostate","prostate-mcrpc"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["therap","nct07611110"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Jevtana","modality":"Cytotoxic chemotherapy (taxane)","mechanism":"Taxane with low P-glycoprotein affinity, active in docetaxel-resistant disease.","approvals":[{"region":"US","year":2010,"indication":"mCRPC after docetaxel"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"cabozantinib","kind":"drug","name":"Cabozantinib","aka":[],"tldr":"A pill that blocks both blood-vessel growth and the MET escape pathway, used in kidney, liver, thyroid and, since 2025, neuroendocrine cancers.","summary":"CELESTIAL: OS 10.2 vs 8.0 months after sorafenib in HCC (HR 0.76). CheckMate 9ER: with nivolumab, first-line RCC. CABINET (2024-25): PFS 13.8 vs 4.4 months in pancreatic NETs and 8.4 vs 3.9 months in extra-pancreatic NETs after prior therapy, leading to FDA approval in March 2025; ESMO 2025 subgroup showed an 81% reduction in progression risk in lung and thymic NETs. COSMIC-312 (with atezolizumab, first-line HCC) improved PFS but not OS.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Cabozantinib","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Cabozantinib"}],"tags":[],"related":[],"indications":["hcc","rcc","neuroendocrine","thyroid"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["cabinet","nct03690388"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["In kidney cancer: CABOSUN (first line versus sunitinib, PFS benefit), METEOR (second line versus everolimus, OS 21.4 versus 16.5 months), CheckMate 9ER (with nivolumab, OS benefit), COSMIC-313 (triplet, no OS gain) and CONTACT-03 (no benefit from adding atezolizumab). The dose is 40 mg daily with nivolumab, and about 65 percent of patients have a grade 3 or higher event; the long half-life of about 99 hours matters when toxicity appears."],"brand":"Cabometyx","modality":"Small-molecule multi-kinase inhibitor (MET, VEGFR2, AXL, RET)","mechanism":"Oral inhibitor of MET, VEGFR2, AXL, RET, KIT and FLT3; MET/AXL inhibition counters anti-VEGF resistance.","approvals":[{"region":"US","year":2012,"indication":"Medullary thyroid cancer (Cometriq)"},{"region":"US","year":2016,"indication":"Advanced RCC"},{"region":"US","year":2019,"indication":"HCC previously treated with sorafenib"},{"region":"US","year":2025,"indication":"Advanced pancreatic and extra-pancreatic neuroendocrine tumours after prior therapy (CABINET)"},{"region":"US","year":2017,"indication":"First-line advanced RCC (CABOSUN)"},{"region":"US","year":2021,"indication":"First-line advanced RCC with nivolumab (CheckMate 9ER)"},{"region":"EU","year":2014,"indication":"Cometriq for medullary thyroid cancer; 21 Mar 2014. Cabometyx (RCC) Sep 2016"}],"mechanismSteps":["Blocks VEGFR2 on endothelium","Blocks MET and AXL, which tumours upregulate under hypoxia to escape anti-VEGF therapy","Reduces invasion and metastasis signalling"],"dosing":{"route":"Oral","schedule":"60 mg daily (Cabometyx tablets)","modifications":"40 mg then 20 mg for intolerance","monitoring":"Blood pressure, liver enzymes, wound healing"},"toxicity":[{"event":"Hand-foot skin reaction","anyGradePct":46,"grade3PlusPct":17,"note":"CELESTIAL"},{"event":"Hypertension","anyGradePct":29,"grade3PlusPct":16,"note":"CELESTIAL"},{"event":"Diarrhoea","anyGradePct":54,"grade3PlusPct":10,"note":"CELESTIAL"}],"access":[],"regulatoryEvents":[{"date":"2025-03-26","type":"approval","region":"US","note":"NET indication on CABINET","source":"https://www.ncf.net/post/2025-highlights-in-neuroendocrine-cancer"}]},{"id":"capecitabine","kind":"drug","name":"Capecitabine","aka":[],"tldr":"Capecitabine (Xeloda) is a tablet form of the chemotherapy fluorouracil. It is a backbone of treatment for bowel cancer and a standard option in advanced breast cancer.","summary":"Capecitabine was approved by the FDA in 1998 for anthracycline- and taxane-resistant metastatic breast cancer and later for adjuvant stage III colon cancer (X-ACT: disease-free survival at least equivalent to bolus fluorouracil and leucovorin), metastatic colorectal cancer, perioperative chemoradiotherapy for rectal cancer and, with docetaxel, for anthracycline-pretreated breast cancer. The EU authorised Xeloda in 2001; it is also approved there for gastric cancer. It is the oral partner in CAPOX and CAPTEM and in the CREATE-X post-neoadjuvant breast regimen. Hand-foot syndrome, diarrhoea and cardiotoxicity are the key toxicities, and DPD deficiency (DPYD variants) causes severe or fatal toxicity, so genotype-guided dosing is increasingly used. Warfarin interaction carries a boxed warning.","status":"approved","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Capecitabine","links":[{"label":"US label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=capecitabine"},{"label":"NCI drug page","url":"https://www.cancer.gov/about-cancer/treatment/drugs/capecitabine"},{"label":"EPAR","url":"https://www.ema.europa.eu/en/medicines/human/EPAR/xeloda"}],"tags":["nci-list","generic"],"related":[],"indications":["breast-her2-positive"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["nct06247995","nct04919226"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Xeloda","modality":"Oral fluoropyrimidine prodrug (antimetabolite)","mechanism":"Converted in three steps, the last by thymidine phosphorylase enriched in tumours, to fluorouracil; FdUMP blocks thymidylate synthase and FUTP is incorporated into RNA.","approvals":[{"region":"US","year":1998,"indication":"Metastatic breast cancer after anthracycline and taxane; later adjuvant and metastatic colorectal cancer, rectal chemoradiotherapy"},{"region":"EU","year":2001,"indication":"Colorectal, gastric and breast cancer"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"choline-c11","kind":"drug","name":"Choline C-11","aka":["[11C]choline"],"tldr":"Choline C-11 was the first PET tracer approved in the United States, in 2012, to find where prostate cancer has come back when PSA rises after treatment; PSMA tracers have now largely replaced it.","summary":"The FDA approved Choline C 11 Injection in September 2012, produced at the Mayo Clinic, for PET imaging of patients with suspected prostate cancer recurrence and non-informative bone scan, CT or MRI, the first approval of a PET agent for prostate cancer. Its 20-minute half-life means it must be made on site with a cyclotron, which confined it to a few centres. From 2020 the PSMA-targeted tracers gallium-68 PSMA-11 and piflufolastat F-18, with higher sensitivity at low PSA and longer half-lives, took over most recurrence imaging, and fluciclovine F-18 offered a distributable amino-acid alternative.","status":"established","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Choline_C-11","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Choline_C-11"},{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=choline%20c%2011"}],"tags":["gap-fill","chembl-universe"],"related":["f-18","ga-68","c-11"],"indications":["prostate"],"sections":[],"technologies":["pet","psma-pet"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Choline C 11 Injection","modality":"PET radiotracer, intravenous","mechanism":"Carbon-11-labelled choline is taken up by cells with high phosphatidylcholine synthesis, including prostate cancer, and imaged by PET within minutes because of the isotope's 20-minute half-life.","approvals":[{"region":"US","year":2012,"indication":"PET imaging of suspected prostate cancer recurrence with non-informative conventional imaging"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"cu-64-dotatate","kind":"drug","name":"Copper-64 dotatate","aka":["64Cu-DOTATATE","Detectnet"],"tldr":"An injectable tracer that sticks to a marker (somatostatin receptor) many neuroendocrine tumours carry. A PET scan afterwards shows where those tumours are, including small deposits that other scans can miss.","summary":"Detectnet (copper Cu 64 dotatate injection) was approved by FDA on 3 September 2020 under NDA 213227, sponsored by RadioMedix and commercialised by Curium, for use with PET to localise somatostatin-receptor-positive neuroendocrine tumours in adults. Approval rested on a US phase 3, reader-masked trial in 63 subjects (42 with known or suspected NETs, 21 healthy volunteers) run by Ebrahim Delpassand and colleagues, which found a diagnostic dose of 148 MBq (4 mCi) gave 100% sensitivity and 96.8% specificity after correcting an initial standard-of-truth misread, with excellent inter-reader agreement and no drug-related serious adverse events.\n\nCopper-64's longer half-life is the main practical advantage over the older gallium-68 tracers (NETSPOT/Ga-68 DOTATATE, Ga-68 DOTATOC): it permits central manufacture and next-day-style logistics, and its lower positron energy gives comparable or slightly better spatial resolution. Reported adverse reactions in the label are nausea, vomiting and flushing, with no listed contraindications. The recommended dose is 148 MBq (4 mCi) IV, with imaging roughly an hour later.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Detectnet (copper Cu 64 dotatate injection)","url":"https://www.accessdata.fda.gov/Drugsatfda_Docs/Label/2020/213227s000lbl.Pdf"},{"label":"FDA approval letter, NDA 213227 (2020)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213227Orig1s000Approv.pdf"},{"label":"Delpassand et al., J Nucl Med 2020: 64Cu-DOTATATE PET/CT pivotal phase 3 trial","url":"https://pubmed.ncbi.nlm.nih.gov/31924723/"}],"tags":["SSTR2","NET imaging","copper-64"],"related":["ga68-dotatate","ga-68-dotatoc","ga-68","cu-64"],"indications":["neuroendocrine","pancreatic-net","small-intestinal-net"],"sections":[],"technologies":["sstr-pet","pet-ct"],"targets":["sstr2"],"drugs":[],"companies":["radiomedix","curium"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Detectnet","modality":"PET tracer","mechanism":"DOTATATE is a somatostatin analogue peptide that binds somatostatin receptor subtype 2 (SSTR2), which is overexpressed on most well-differentiated neuroendocrine tumour cells. Labelling it with copper-64 rather than gallium-68 gives a longer physical half-life (12.7 hours versus 68 minutes), which lets a single cyclotron batch supply multiple patients and imaging sites over the course of a working day without an on-site generator.","approvals":[{"region":"US","year":2020,"indication":"PET localisation of somatostatin receptor-positive neuroendocrine tumours in adult patients"}],"mechanismSteps":[],"dosing":{"route":"Intravenous bolus injection","schedule":"148 MBq (4 mCi), imaging approximately 60 minutes after injection","source":"https://www.accessdata.fda.gov/Drugsatfda_Docs/Label/2020/213227s000lbl.Pdf"},"toxicity":[{"event":"Nausea","source":"https://www.accessdata.fda.gov/Drugsatfda_Docs/Label/2020/213227s000lbl.Pdf"},{"event":"Vomiting","source":"https://www.accessdata.fda.gov/Drugsatfda_Docs/Label/2020/213227s000lbl.Pdf"},{"event":"Flushing","source":"https://www.accessdata.fda.gov/Drugsatfda_Docs/Label/2020/213227s000lbl.Pdf"}],"access":[],"regulatoryEvents":[]},{"id":"cu-64-sar-bispsma","kind":"drug","name":"Copper-64 SAR-bisPSMA","aka":["64Cu-SAR-bisPSMA","64Cu-bisPSMA"],"tldr":"An experimental PET tracer for prostate cancer that binds the same target as approved PSMA scans (PSMA) but, because its radioactive tag lasts longer, can be re-imaged a day later to catch small deposits the first picture missed. It is not yet approved for sale.","summary":"64Cu-SAR-bisPSMA is Clarity Pharmaceuticals' diagnostic partner to its therapeutic 67Cu-SAR-bisPSMA, developed as a Targeted Copper Theranostic pair. In the phase 1 PROPELLER trial (NCT04839367, 30 men with intermediate-to-high-risk untreated prostate cancer), the optimal 200 MBq dose detected primary prostate cancer in 100% and 85.7% of patients by two independent readers, versus 77.8% and 83.3% for same-patient 68Ga-PSMA-11, with significantly higher SUVmax and tumour-to-background ratio (p<0.001 for both readers). In the Co-PSMA trial (NCT06907641, 50 men with biochemical recurrence after prostatectomy), 24-hour 64Cu-SAR-bisPSMA imaging found more than double the per-patient lesion count of same-day 68Ga-PSMA-11 (mean 1.26 vs 0.48 lesions, p<0.0001) and changed management in 44% of patients, published in European Urology in 2026.\n\nThe US FDA granted 64Cu-SAR-bisPSMA fast-track designation in August 2024 for PET imaging of PSMA-positive prostate cancer with suspected metastasis in patients eligible for initial definitive therapy. A registrational phase 3 trial, CLARIFY (NCT06056830), is evaluating same-day and next-day imaging ahead of radical prostatectomy. The therapeutic isotope pairing, 67Cu-SAR-bisPSMA, is being tested in the SECuRE trial (NCT04868604) for PSMA-expressing metastatic castration-resistant prostate cancer; both 64Cu- and 67Cu-SAR-bisPSMA remain unregistered products not yet assessed for approval by FDA or Australia's TGA, per the company's own disclosures.","status":"phase-3","asOf":"2026-09-22","links":[{"label":"Lengyelova, Wong, Lenzo, Parker, Emmett; JCO 2023: 64Cu-SAR-bisPSMA (PROPELLER) PET imaging in confirmed prostate cancer","url":"https://ascopubs.org/doi/10.1200/JCO.2023.41.16_suppl.5039"},{"label":"Co-PSMA trial, European Urology 2026: prospective comparison of 64Cu-SAR-bisPSMA vs 68Ga-PSMA-11 for biochemical recurrence","url":"https://pubmed.ncbi.nlm.nih.gov/41904043/"},{"label":"ClinicalTrials.gov NCT04868604 (SECuRE)","url":"https://clinicaltrials.gov/study/NCT04868604"}],"tags":["PSMA","copper-64","theranostic pair","investigational"],"related":["tc-99m-psma-imaging","ga-68","cu-64","cu-67"],"indications":["prostate-high-risk","prostate-bcr","prostate-mcrpc"],"sections":[],"technologies":["psma-pet","pet-ct"],"targets":["psma"],"drugs":[],"companies":["clarity-pharmaceuticals"],"institutions":[],"pathways":[],"terms":[],"trials":["nct04868604"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"A bivalent small-molecule ligand carrying two PSMA-binding moieties on a single sarcophagine (SAR) chelator backbone, labelled with copper-64. The bivalent design and copper-64's 12.7-hour half-life allow same-day and next-day imaging from a single injection, and Clarity Pharmaceuticals reports two- to three-fold higher tumour uptake (SUVmax) than the standard-of-care 68Ga-PSMA-11 in head-to-head comparisons.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"dexrazoxane","kind":"drug","name":"Dexrazoxane","aka":["Cardioxane","Savene"],"tldr":"Dexrazoxane protects the heart from the cumulative damage of doxorubicin in women with metastatic breast cancer who need to keep receiving it, and, as Totect, limits tissue destruction when an anthracycline leaks out of a vein.","summary":"Dexrazoxane (Zinecard) was approved in May 1995 to reduce the incidence and severity of doxorubicin cardiomyopathy in women with metastatic breast cancer who have received a cumulative 300 mg/m2 and will continue doxorubicin, on randomised trials that markedly reduced cardiac events; it is not used from the start of treatment because of an early signal of reduced response, later not confirmed. Totect was approved in 2007 for anthracycline extravasation, given within six hours on three consecutive days, on two single-arm European studies in which surgery was avoided in the great majority. Dexrazoxane is also used in paediatric leukaemia and lymphoma protocols to protect against late cardiotoxicity, an area where long-term Children's Oncology Group follow-up has been reassuring about secondary malignancy. Myelosuppression adds to that of chemotherapy.","status":"approved","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Dexrazoxane","links":[{"label":"US label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=dexrazoxane"},{"label":"NCI drug page","url":"https://www.cancer.gov/about-cancer/treatment/drugs/dexrazoxanehydrochloride"}],"tags":["nci-list","supportive"],"related":[],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["pfizer"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Zinecard / Totect","modality":"Cardioprotectant and extravasation antidote (bisdioxopiperazine)","mechanism":"Cyclic EDTA derivative hydrolysed intracellularly to a metal chelator that removes iron from anthracycline-iron complexes, limiting free-radical cardiac injury; also a catalytic topoisomerase II inhibitor, which underlies its action against extravasation injury.","approvals":[{"region":"US","year":1995,"indication":"Reduction of doxorubicin cardiomyopathy in women with metastatic breast cancer after 300 mg/m2 cumulative dose (Zinecard)"},{"region":"US","year":2007,"indication":"Anthracycline extravasation (Totect)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"docetaxel","kind":"drug","name":"Docetaxel","aka":[],"tldr":"The first chemotherapy to extend life in prostate cancer (2004), now part of triplet therapy at first metastatic diagnosis.","summary":"Docetaxel is a taxane that stabilises microtubules and arrests dividing cells; in prostate cancer it also disrupts androgen receptor nuclear trafficking. It was the first chemotherapy to extend life in metastatic castration-resistant prostate cancer (TAX 327, 2004) and later moved to first metastatic diagnosis: CHAARTED (OS 57.6 versus 44.0 months, HR 0.61) and STAMPEDE showed an overall survival benefit in high-volume hormone-sensitive disease, and PEACE-1 and ARASENS built triplets by adding abiraterone or darolutamide. It is also widely used in breast, lung, gastric and head and neck cancers. Neutropenia, neuropathy and fluid retention limit its use in frail patients, and whether men with low-volume metastatic disease gain anything from it remains contested. For a newcomer, it is the workhorse chemotherapy given every three weeks across many cancers.","status":"approved","asOf":"2026-09-06","wikipedia":"https://en.wikipedia.org/wiki/Docetaxel","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Docetaxel"}],"tags":[],"related":[],"indications":["prostate","prostate-mhspc","prostate-mcrpc"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["chaarted","stampede","nct06520345","nct07590934"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Taxotere (generic)","modality":"Cytotoxic chemotherapy (taxane)","mechanism":"Microtubule stabilisation; also disrupts AR nuclear trafficking.","approvals":[{"region":"US","year":1996,"indication":"Locally advanced or metastatic breast cancer after chemotherapy (Taxotere, NDA 020449)"},{"region":"US","year":2004,"indication":"Metastatic CRPC (with prednisone)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"donafenib","kind":"drug","name":"Donafenib","aka":[],"tldr":"Donafenib is a Chinese redesign of sorafenib that lived longer than the original in a head-to-head liver cancer trial and is approved in China as a first-line option.","summary":"Zelgen's donafenib was approved by the NMPA in June 2021 for first-line unresectable hepatocellular carcinoma on the ZGDH3 trial (668 patients: median overall survival 12.1 versus 10.3 months with sorafenib, hazard ratio 0.83; Journal of Clinical Oncology 2021), the first drug to beat sorafenib on survival in this setting. Radioiodine-refractory differentiated thyroid cancer followed in 2022. A modest gain, but a first for a Chinese company and a model of incremental chemistry (deuteration) turned into an approval.","status":"approved","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Donafenib","links":[{"label":"Suzhou Zelgen Biopharmaceuticals","url":"https://www.zelgen.com/en/"},{"label":"ZGDH3 (J Clin Oncol 2021)","url":"https://doi.org/10.1200/JCO.20.02672"},{"label":"NMPA (National Medical Products Administration)","url":"https://www.nmpa.gov.cn"}],"tags":["china"],"related":[],"indications":["hcc","thyroid"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Zepsun","code":"CM4307","modality":"Small-molecule multi-kinase inhibitor (deuterated sorafenib)","mechanism":"Deuterium-substituted analogue of sorafenib inhibiting RAF kinases and VEGFR/PDGFR; deuteration slows metabolism and raises exposure.","approvals":[{"region":"China","year":2021,"indication":"First-line unresectable hepatocellular carcinoma (ZGDH3)"},{"region":"China","year":2022,"indication":"Radioiodine-refractory differentiated thyroid cancer"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"durvalumab","kind":"drug","name":"Durvalumab","aka":[],"tldr":"A PD-L1 blocker that became standard after chemoradiation for stage III lung cancer, and now in bladder, biliary, and gastric cancers.","summary":"PACIFIC (unresectable stage III NSCLC), ADRIATIC (limited-stage SCLC, 2024), TOPAZ-1 (biliary tract), HIMALAYA (HCC with tremelimumab), NIAGARA (perioperative muscle-invasive bladder cancer, 2025), MATTERHORN (perioperative gastric, 2025), and Q2 2026 high-risk non-muscle-invasive bladder cancer with BCG (POTOMAC). Partner of Dato-DXd in TROPION-Breast05.","status":"approved","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Durvalumab","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Durvalumab"}],"tags":[],"related":[],"indications":["sclc","hcc","hcc-intermediate"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["astrazeneca"],"institutions":[],"pathways":[],"terms":[],"trials":["nct05063565","nct06040099"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Imfinzi","modality":"Monoclonal antibody (anti-PD-L1)","mechanism":"Human IgG1 anti-PD-L1 with reduced Fc effector function.","approvals":[{"region":"US","year":2017,"indication":"Locally advanced or metastatic urothelial carcinoma after platinum (accelerated; indication withdrawn 2021)"},{"region":"US","year":2018,"indication":"Unresectable stage III NSCLC after chemoradiation"},{"region":"US","year":2026,"indication":"High-risk NMIBC with BCG"}],"mechanismSteps":["Antibody binds PD-L1","PD-1/PD-L1 engagement between T cell and tumour is blocked","Exhausted tumour-reactive T cells regain effector function","Interferon-γ and cytotoxic granules are released at the tumour","Tumour cells are killed; memory T cells persist"],"dosing":{"route":"IV infusion","schedule":"10 mg/kg every 2 weeks or 1,500 mg every 4 weeks (≥30 kg); up to 12 months after chemoradiation in stage III NSCLC","modifications":"Hold for grade 2 pneumonitis; discontinue for grade 3-4","monitoring":"Respiratory symptoms after chemoradiation, thyroid, LFTs, creatinine","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3"},"toxicity":[{"event":"Pneumonitis (any cause, PACIFIC)","anyGradePct":18.3,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3","note":"vs 12.8% placebo; 1.1% fatal"},{"event":"Cough","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3","note":"PACIFIC; all-grade ≥20%"},{"event":"Fatigue","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3","note":"PACIFIC; all-grade ≥20%"},{"event":"Radiation pneumonitis","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3","note":"PACIFIC; all-grade ≥20%"},{"event":"Upper respiratory infection","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3","note":"PACIFIC; all-grade ≥20%"},{"event":"Dyspnoea","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3","note":"PACIFIC; all-grade ≥20%"},{"event":"Rash","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8baba4ea-2855-42fa-9bd9-5a7548d4cec3","note":"PACIFIC; all-grade ≥20%"}],"access":[{"country":"US","reimbursement":"Medicare Part B (physician-administered); commercial plans per formulary","assistance":"https://www.astrazeneca-us.com/medicines/access-360","source":"https://www.cms.gov/medicare/payment/part-b-drugs/asp-pricing-files","asOf":"2026-09-06"},{"country":"UK","reimbursement":"NICE: recommended after chemoradiation in stage III NSCLC (TA798), biliary tract cancer, limited-stage SCLC, perioperative bladder and gastric cancer","source":"https://www.nice.org.uk/guidance/published?ngt=Technology%20appraisal%20guidance","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2017-05-01","type":"approval","region":"US","note":"Urothelial carcinoma (accelerated; later withdrawn 2021)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2018-02-16","type":"approval","region":"US","note":"Unresectable stage III NSCLC after chemoradiation (PACIFIC)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2020-03-27","type":"approval","region":"US","note":"Extensive-stage SCLC with chemotherapy (CASPIAN)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2022-09-02","type":"approval","region":"US","note":"Biliary tract cancer with chemotherapy (TOPAZ-1)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2022-10-21","type":"approval","region":"US","note":"HCC with tremelimumab (HIMALAYA)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2024-12-04","type":"approval","region":"US","note":"Limited-stage SCLC after chemoradiation (ADRIATIC)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2025-03-28","type":"approval","region":"US","note":"Perioperative muscle-invasive bladder cancer (NIAGARA)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2025-11","type":"approval","region":"US","note":"Perioperative gastric/GEJ cancer with FLOT (MATTERHORN)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2026-05-28","type":"approval","region":"US","note":"High-risk non-muscle-invasive bladder cancer with BCG (POTOMAC)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-durvalumab-combination-bacillus-calmette-guerin-high-risk-non-muscle-invasive-bladder"}]},{"id":"enzalutamide","kind":"drug","name":"Enzalutamide","aka":[],"tldr":"Enzalutamide is a second-generation androgen-receptor blocker that stops the receptor binding testosterone, entering the nucleus and switching on genes. It is approved at every stage of advanced prostate cancer, from rising PSA after surgery to castration-resistant disease, and fatigue, falls and memory problems are its main drawbacks.","summary":"Enzalutamide is a second-generation androgen receptor antagonist that blocks ligand binding, nuclear translocation and DNA binding, giving more complete AR blockade than older antiandrogens. It is approved across every stage of advanced prostate cancer: AFFIRM and PREVAIL (mCRPC), PROSPER (nmCRPC), ARCHES and ENZAMET (mHSPC, overall survival benefit; ARCHES OS HR 0.66) and EMBARK (high-risk biochemical recurrence, 2023, metastasis-free survival HR 0.42 with leuprolide). It is the partner in TALAPRO-2 (talazoparib) and the MEVPRO trials (mevrometostat), so the next generation of combinations is built on it. Fatigue, falls and cognitive effects are the main toxicities, which is why darolutamide or apalutamide is sometimes preferred in frail men. For a newcomer, enzalutamide is the most widely used androgen-receptor blocker, from rising PSA after surgery to late-stage disease.","status":"approved","asOf":"2026-09-27","wikipedia":"https://en.wikipedia.org/wiki/Enzalutamide","links":[{"label":"FDA supplement approval letter: Xtandi NDA 203415/S-026 and NDA 213674/S-016 (EMBARK overall survival), 24 July 2026","url":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2026/203415Orig1s026;213674Orig1s016ltr.pdf"},{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Enzalutamide"}],"tags":[],"related":[],"indications":["prostate","prostate-mhspc","prostate-nmcrpc","prostate-mcrpc","prostate-bcr"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["pfizer"],"institutions":[],"pathways":[],"terms":["mcrpc-mhspc"],"trials":["embark","nct06520345","nct07611110"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Xtandi","modality":"Small-molecule AR antagonist","mechanism":"Second-generation AR antagonist blocking ligand binding, nuclear translocation, and DNA binding.","approvals":[{"region":"US","year":2012,"indication":"mCRPC after docetaxel (pre-chemo 2014)"},{"region":"US","year":2018,"indication":"Non-metastatic CRPC"},{"region":"US","year":2019,"indication":"mHSPC (ARCHES)"},{"region":"US","year":2023,"indication":"High-risk biochemical recurrence (EMBARK)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2026-07-24","type":"label-change","region":"US","note":"US Prescribing Information updated with overall survival data from EMBARK (NDA 203415/S-026, NDA 213674/S-016; efficacy labelling change with clinical data)","source":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2026/203415Orig1s026;213674Orig1s016ltr.pdf"}]},{"id":"everolimus","kind":"drug","name":"Everolimus","aka":[],"tldr":"An mTOR-blocking pill that doubled progression-free time with exemestane in 2012 and is now paired with the oral SERD giredestrant.","summary":"Everolimus is a rapalog that binds FKBP12 and allosterically inhibits mTORC1, a growth-signalling hub downstream of PI3K and AKT. It is approved in HR-positive breast cancer with exemestane after non-steroidal aromatase inhibitor failure, in progressive pancreatic, lung and GI neuroendocrine tumours, and in advanced RCC after sunitinib or sorafenib. BOLERO-2 showed PFS of 7.8 versus 3.2 months for everolimus plus exemestane versus exemestane alone, with no OS benefit; RADIANT-3 and RADIANT-4 showed PFS of 11.0 versus 4.6 and 3.9 months in NETs. Stomatitis (mitigated by dexamethasone mouthwash, SWISH), pneumonitis and hyperglycaemia are the main toxicities. evERA (2025) revived it as the partner of giredestrant after CDK4/6 inhibitors; it is the comparator beaten in LITESPARK-005 and COMPETE. For a newcomer, it is a growth-pathway pill with several niches rather than one dominant use.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Everolimus","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Everolimus"}],"tags":[],"related":[],"indications":["rcc","neuroendocrine"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["novartis"],"institutions":[],"pathways":[],"terms":[],"trials":["nct04919226","radiant-3-4","compete"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["In neuroendocrine tumours: RADIANT-3 (2011) gave PFS 11.0 versus 4.6 months in pancreatic NETs and RADIANT-4 (2016) PFS 11.0 versus 3.9 months in lung and GI NETs; it is now the comparator that 177Lu-edotreotide beat in COMPETE. In RADIANT-3 stomatitis affected 64 percent (7 percent grade 3 or higher), rash 49 percent and pneumonitis 17 percent; dexamethasone mouthwash (SWISH) prevents most stomatitis.","In kidney cancer: RECORD-1 (2008) gave PFS 4.9 versus 1.9 months against placebo after a VEGF-TKI, making everolimus the second-line standard from 2009; it has since been beaten by nivolumab (CheckMate 025), cabozantinib (METEOR), lenvatinib plus everolimus (Study 205) and belzutifan (LITESPARK-005), and is now mostly a comparator arm and a partner for lenvatinib at 5 mg daily. Feedback activation of AKT limits its cytostatic effect."],"brand":"Afinitor","modality":"Small-molecule mTOR inhibitor","mechanism":"Allosteric mTORC1 inhibitor (rapalog) via FKBP12.","approvals":[{"region":"US","year":2012,"indication":"HR+/HER2- advanced breast cancer with exemestane after NSAI failure"},{"region":"US","year":2011,"indication":"Progressive pancreatic NETs"},{"region":"US","year":2016,"indication":"Progressive non-functional lung and GI NETs"},{"region":"US","year":2009,"indication":"Advanced RCC after sunitinib or sorafenib"}],"mechanismSteps":[],"dosing":{"route":"Oral","schedule":"10 mg once daily","modifications":"5 mg for stomatitis or pneumonitis","monitoring":"Glucose, lipids, pneumonitis symptoms; steroid mouthwash prophylaxis"},"toxicity":[{"event":"Stomatitis","anyGradePct":59,"grade3PlusPct":8},{"event":"Pneumonitis","anyGradePct":16,"grade3PlusPct":3},{"event":"Hyperglycaemia","anyGradePct":14,"grade3PlusPct":5}],"access":[],"regulatoryEvents":[]},{"id":"fap-2286","kind":"drug","name":"FAP-2286 (177Lu / 68Ga)","aka":[],"tldr":"A FAP-targeted theranostic pair: one version images almost any solid tumour, the other treats it with radiation.","summary":"FAP-2286 is a theranostic pair: a cyclic peptide that binds fibroblast activation protein (FAP), linked to a DOTA chelator carrying 68Ga for PET imaging or 177Lu for beta therapy. FAP sits on cancer-associated fibroblasts in the stroma of most solid tumours rather than on cancer cells, so one agent can image and irradiate many tumour types, and the cyclic peptide gives longer tumour retention than the FAPI small molecules used for imaging. Clovis Oncology developed it until its 2022 bankruptcy; Novartis then acquired it via 3B Pharmaceuticals. The 177Lu-FAP-2286 LuMIERE phase 1/2 trial is dose-escalating in cycles every 6 weeks with pancreatic, sarcoma and breast cohorts. For a newcomer: a radioligand aimed at the scaffolding around tumours rather than the tumour cells.","status":"phase-2","asOf":"2026-09-04","links":[{"label":"ClinicalTrials.gov: trials of FAP-2286 (177Lu / 68Ga)","url":"https://clinicaltrials.gov/search?intr=FAP-2286"}],"tags":[],"related":["ga-68","lu-177"],"indications":[],"sections":[],"technologies":["fapi-pet","radioligand-therapy"],"targets":["fap"],"drugs":[],"companies":["novartis"],"institutions":[],"pathways":[],"terms":[],"trials":["nct05939414","nct06520345","nct07219238","nct05413850","nct06894511","nct05142696","nct04939610"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"FAP-2286","modality":"Theranostic pair (peptide radioligand)","mechanism":"Cyclic peptide FAP binder with DOTA chelator for 68Ga (imaging) or 177Lu (therapy).","approvals":[],"mechanismSteps":["Radioligand circulates and binds FAP on cancer-associated fibroblasts on tumour cells","Ligand is internalised or retained at the membrane","Beta emissions deposit energy within a short range","Clustered DNA double-strand breaks form in the tumour cell and its neighbours (crossfire)","Cells die; unbound ligand is cleared via the kidneys"],"dosing":{"route":"IV infusion (177Lu) or injection (68Ga)","schedule":"LuMIERE phase 1/2 dose escalation, cycles every 6 weeks","monitoring":"Blood counts, renal function","source":"https://clinicaltrials.gov/study/NCT04939610"},"toxicity":[{"event":"Anaemia"},{"event":"Thrombocytopenia"},{"event":"Fatigue"},{"event":"Nausea"}],"access":[{"country":"US","reimbursement":"Investigational","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2023-01","type":"filing","region":"US","note":"Novartis acquires rights after Clovis bankruptcy","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},{"id":"florastamin-f18","kind":"drug","name":"Florastamin F-18","aka":["18F-florastamin","ProstaView","Prostaview Injection","florastamine","flortastamine F-18"],"tldr":"Florastamin is FutureChem's fluorine-18 PSMA PET tracer, and the first prostate cancer diagnostic developed in South Korea to be approved there — Korea's 43rd domestically developed new drug.","summary":"FutureChem, a Seoul radiopharmaceutical company, developed florastamin (FC303) as a fluorine-18 PSMA ligand for PET imaging of prostate cancer. Korea's Ministry of Food and Drug Safety approved it on 30 April 2026 as ProstaView injection, the country's 43rd domestically developed new drug and its first home-grown prostate cancer diagnostic; first commercial sales followed on 20 August 2026, the four-month gap being the reimbursement notice and hospital code registration every new Korean drug waits through. The company romanises the brand as both ProstaView and Prostaview and the ingredient appears as florastamin, florastamine and, in one wire report, flortastamine.\n\nThe registrational evidence is a domestic phase 3 trial at 11 institutions in men whose conventional imaging suggested recurrence or metastasis. Positive predictive value, the primary endpoint, was 86.96 per cent with a 95 per cent confidence interval lower bound of 79.01, against a pre-specified benchmark of 60.6; the CT, MRI and bone scans those same patients had already had returned about 60.16 per cent. A separate prospective study in 59 men with suspected intermediate-risk disease (Clinical Nuclear Medicine, 2025) put sensitivity at 72.4 per cent and specificity at 83.3 per cent against biopsy, with multiparametric MRI more sensitive at 89.7 per cent but less specific at 66.7 per cent and the same overall accuracy of 78 per cent — a fair description of what PSMA PET adds to MRI rather than replaces.\n\nRegistered phase 3 trials also cover initial staging of high-risk prostate cancer, the setting where gallium-68 PSMA-11 and piflufolastat are already approved in the United States and Europe. The approval matters beyond Korea because it is the diagnostic half of a domestic theranostic pair: FutureChem's lutetium-177 therapy FC705 (ludotadipep) targets the same antigen and is in phase 3 in Korea, so the approved tracer is the selection tool that therapy will be filed with.","status":"approved","asOf":"2026-09-22","links":[{"label":"FutureChem wins approval for Korea's first prostate cancer diagnostic (Seoul Economic Daily, English)","url":"https://en.sedaily.com/finance/2026/05/04/futurechem-wins-approval-for-koreas-first-prostate-cancer"},{"label":"First sales, with the 30 April 2026 approval date (Edaily, English)","url":"https://en.edaily.co.kr/news/eda202608205175/"},{"label":"Diagnostic accuracy of 18F-florastamin PET/CT in intermediate-risk suspected prostate cancer (Clin Nucl Med, 2025)","url":"https://doi.org/10.1097/RLU.0000000000005798"},{"label":"18F-florastamin PET/CT in men with clinical suspicion of prostate cancer (Prostate International, 2025)","url":"https://doi.org/10.1016/j.prnil.2025.07.001"},{"label":"ClinicalTrials.gov: trials of Florastamin F-18","url":"https://clinicaltrials.gov/search?intr=FC303"}],"tags":["diagnostic","psma","korea","ctgov-ingest"],"related":["ksnm","nuclear-medicine-and-molecular-imaging","f-18","prostate-bcr","ga-68","lu-177"],"indications":["prostate"],"sections":[],"technologies":["psma-pet","pet"],"targets":["psma"],"drugs":[],"companies":["futurechem"],"institutions":[],"pathways":[],"terms":[],"trials":["nct05936658","nct05004285","nct06754085"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2, curated); Korean approval read from the company's announcement in the English editions of Seoul Economic Daily and Edaily","editedOn":"2026-09-22"},"brand":"ProstaView","code":"FC303","modality":"PSMA-targeted PET radiotracer, fluorine-18","mechanism":"A fluorine-18-labelled ligand of prostate-specific membrane antigen that lights up prostate cancer on PET wherever it has spread.","approvals":[{"region":"South Korea","year":2026,"indication":"PET imaging of PSMA-positive lesions in men with prostate cancer whose existing imaging suggests recurrence or metastasis","note":"MFDS marketing approval 30 April 2026; Korea's 43rd domestically developed new drug"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2026-04-30","type":"approval","region":"South Korea","note":"MFDS marketing approval as Korea's 43rd domestically developed new drug","source":"https://en.sedaily.com/finance/2026/05/04/futurechem-wins-approval-for-koreas-first-prostate-cancer"}]},{"id":"f-18-florbetaben","kind":"drug","name":"Florbetaben F-18","aka":["Neuraceq"],"tldr":"A PET scan tracer that lights up amyloid plaques in the brain, helping doctors work out whether memory problems are due to Alzheimer's disease and whether the patient can have amyloid-lowering treatment.","summary":"Florbetaben F-18 (Neuraceq, originally Piramal, now Life Molecular Imaging/Lantheus) was FDA-approved in March 2014 and EMA-approved in February 2014, for PET imaging of the brain to estimate beta-amyloid neuritic plaque density in adults with cognitive impairment being evaluated for AD and other causes of cognitive decline. As with florbetapir and flutemetamol, the current US label has been updated to add selection of patients for amyloid beta-directed therapy as a second indication.\n\nThe recommended dose is 300 MBq (8.1 mCi) given as a slow intravenous bolus (6 seconds/mL) in up to 10 mL, maximum mass dose 30 micrograms; PET imaging in the US label starts 45 to 130 minutes post-injection (commonly around 90 minutes), and the EU posology allows 240-360 MBq with the target at 300 MBq. Effective dose from a 300 MBq administration is about 5.8 mSv.\n\nVisual interpretation looks for loss of the normal grey-white matter contrast from increased cortical tracer retention; florbetaben has its own validated linear conversion to the Centiloid scale, and the 2024 EMA/CHMP qualification opinion on the Centiloid measure discusses florbetaben-specific data showing that values above about 35 CL indicate established amyloid pathology while values below about 20 CL are compatible with a negative visual read, with 20-35 CL an ambiguous zone. Neuraceq sits in the same US clinical-use and Medicare-coverage landscape as the other amyloid tracers: appropriate for diagnostic work-up in uncertain cognitive impairment and for confirming eligibility for anti-amyloid antibody therapy per the 2025 SNMMI/Alzheimer's Association appropriate use criteria, with Medicare coverage now determined locally following the October 2023 retirement of the national coverage determination.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Neuraceq (florbetaben F 18 injection)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2026/204677s041lbl.pdf"},{"label":"EMA EPAR: Neuraceq","url":"https://www.ema.europa.eu/en/medicines/human/EPAR/neuraceq"},{"label":"EMA CHMP: qualification opinion for Centiloid measure of amyloid PET (25 June 2024)","url":"https://www.ema.europa.eu/system/files/documents/other/qualification-opinion-centiloid-measure-amyloid-pet-quantify-brain-amyloid-deposition-en.pdf"},{"label":"CMS: decision memo removing the amyloid PET national coverage determination (NCA-CAL 308)","url":"https://www.cms.gov/medicare-coverage-database/view/ncacal-decision-memo.aspx?proposed=N&ncaid=308"}],"tags":["amyloid PET","diagnostic","neurology"],"related":["alzheimers-disease","f-18-florbetapir","f-18-flutemetamol","lantheus","f-18"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Neuraceq","modality":"PET tracer","mechanism":"A fluorine-18 labelled stilbene derivative that binds fibrillar beta-amyloid plaques in cortical grey matter, giving a PET signal proportional to plaque density.","approvals":[{"region":"US","year":2014,"indication":"PET imaging of the brain to estimate beta-amyloid neuritic plaque density in adults with cognitive impairment being evaluated for AD and other causes of cognitive decline"},{"region":"EU","year":2014,"indication":"PET imaging of beta-amyloid neuritic plaque density in adults with cognitive impairment being evaluated for Alzheimer's disease and other causes of cognitive impairment"}],"mechanismSteps":[],"dosing":{"route":"Intravenous slow bolus (6 sec/mL)","schedule":"300 MBq (8.1 mCi) single dose in up to 10 mL; PET imaging roughly 45-130 minutes after injection (US label)","monitoring":"Visual read of cortical grey-white contrast; tracer-specific Centiloid conversion available for quantification","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2026/204677s041lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"f-18-florbetapir","kind":"drug","name":"Florbetapir F-18","aka":["Amyvid","18F-AV-45"],"tldr":"A PET scan tracer that shows whether a patient's brain contains the sticky amyloid protein clumps linked to Alzheimer's disease, and whether they qualify for amyloid-lowering drugs.","summary":"Florbetapir F-18 (Amyvid, Eli Lilly) was the first amyloid PET tracer approved by the FDA, in April 2012, for imaging beta-amyloid neuritic plaque density in adults with cognitive impairment being evaluated for Alzheimer's disease (AD) and other causes of cognitive decline. In June 2025 the FDA approved a label update adding a second indication: selection of patients who are candidates for amyloid-beta-directed therapy, reflecting the arrival of approved anti-amyloid antibodies. A negative scan indicates sparse to no neuritic plaques and reduces the likelihood that AD explains the impairment; a positive scan indicates moderate to frequent plaques, a pattern also seen in some cognitively normal older adults, so it does not by itself establish an AD diagnosis and is meant to be used alongside full clinical evaluation.\n\nThe recommended dose is 370 MBq (10 mCi) as a single intravenous bolus in up to 10 mL, followed by a saline flush, with 10-minute PET images acquired approximately 30 to 50 minutes after injection. The maximum mass dose is 50 micrograms. Effective dose from a 370 MBq administration is about 7 mSv in an adult. Reading is by visual assessment of cortical grey-white contrast loss by a trained reader; quantification against the Centiloid scale can be used alongside the visual read, per the 2025 label update, and is the metric used to track amyloid clearance during anti-amyloid antibody therapy.\n\nIn the clinical pathway defined by the 2025 SNMMI/Alzheimer's Association appropriate use criteria, amyloid PET is rated 'appropriate' both for diagnostic clarification in patients with an uncertain aetiology after specialist assessment and, with the highest confidence rating, for determining eligibility for an approved amyloid-targeting therapy such as lecanemab or donanemab. In the United States, Medicare coverage of amyloid PET is no longer restricted: CMS retired the national coverage determination at 42 CFR 220.6.20 effective 13 October 2023, ending the prior coverage-with-evidence-development framework and the one-scan-per-lifetime limit, and coverage decisions (including for repeat scans to document plaque clearance) now sit with local Medicare Administrative Contractors rather than a single national rule.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Amyvid (florbetapir F 18 injection), 2025 revision","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/202008s046lbl.pdf"},{"label":"Eli Lilly: FDA approves updated Amyvid label for treatment selection (25 June 2025)","url":"https://investor.lilly.com/news-releases/news-release-details/fda-approves-updated-label-lillys-amyvid-florbetapir-f-18"},{"label":"CMS: decision memo removing the amyloid PET national coverage determination (NCA-CAL 308)","url":"https://www.cms.gov/medicare-coverage-database/view/ncacal-decision-memo.aspx?proposed=N&ncaid=308"},{"label":"SNMMI/Alzheimer's Association: updated appropriate use criteria for amyloid and tau PET (2025)","url":"https://jnm.snmjournals.org/content/early/2025/01/07/jnumed.124.268756"}],"tags":["amyloid PET","diagnostic","neurology"],"related":["alzheimers-disease","f-18-flutemetamol","f-18-florbetaben","f-18-flortaucipir","eli-lilly","f-18"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Amyvid","modality":"PET tracer","mechanism":"A fluorine-18 labelled stilbene derivative that binds to fibrillar amyloid-beta neuritic plaques in the brain; the F-18 positron signal is detected by PET, giving a picture of cortical amyloid burden rather than blood flow or metabolism.","approvals":[{"region":"US","year":2012,"indication":"PET imaging of the brain to estimate beta-amyloid neuritic plaque density in adults with cognitive impairment being evaluated for AD and other causes of cognitive decline"},{"region":"US","year":2025,"indication":"Label update adding selection of patients indicated for amyloid beta-directed therapy"}],"mechanismSteps":[],"dosing":{"route":"Intravenous bolus","schedule":"370 MBq (10 mCi) single dose in up to 10 mL, followed by ~10 mL saline flush; PET imaging 30-50 minutes after injection","monitoring":"Visual read of cortical uptake pattern by a trained reader; quantitative Centiloid analysis may be used alongside the visual read","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/202008s046lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"f-18-fet","kind":"drug","name":"Floretyrosine F-18 (FET)","aka":["18F-FET","O-(2-[18F]fluoroethyl)-L-tyrosine","Pixclara","TLX101-Px"],"tldr":"A brain-tumour PET tracer that shows where active tumour tissue is by how much it grabs a labelled amino acid, which helps tell a true regrowing tumour apart from scan changes caused by past treatment. Approved by the FDA in September 2026, the first scan of its kind cleared for this use in the US.","summary":"Pixclara (floretyrosine F 18, 18F-FET) was approved by FDA on 11 September 2026 (the PDUFA goal date), after an initial complete response letter in April 2025 requesting additional confirmatory clinical evidence and a resubmission by Telix in March 2026. It is indicated for use with PET to differentiate recurrent or progressive glioma from treatment-related change, alongside other diagnostic evaluations, in adults and children from 1 month of age -- making it the first FDA-approved radiopharmaceutical imaging drug for glioma in the US. Safety was assessed in 382 glioma patients; the only adverse reaction at or above 0.5% incidence was headache, with nausea, injection-site reaction, fatigue and malaise each occurring in under 0.5%.\n\nFET-PET has been used in Europe and recommended by joint EANM/EANO/RANO/SNMMI guidelines for glioma imaging for over a decade, well ahead of US approval: recommended adult activity is 185-200 MBq, with a tumour-to-brain SUV ratio threshold of roughly 1.6-1.8 used to define biological tumour volume, and a maximum tumour-to-brain ratio of at least 2.5 associated with a 98% positive predictive value for neoplasm in newly diagnosed lesions. The Pixclara US label sets the adult dose at 185-259 MBq (5-7 mCi) and a paediatric weight-based dose from 1 month of age. The agent remains in a phase 3 registrational study for a possible brain-metastases indication, which is not yet part of the approved US label.","status":"approved","asOf":"2026-09-27","links":[{"label":"Drugs@FDA: NDA 218592, Pixclara (floretyrosine F 18)","url":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=218592"},{"label":"Pixclara (floretyrosine F 18) US Prescribing Information, Telix Pharmaceuticals","url":"https://telixpharma.com/wp-content/uploads/2026/09/USPI_PIXCLARA_Sep2026.pdf"},{"label":"Telix press release: FDA approves Pixclara, 14 September 2026","url":"https://telixpharma.com/news-views/fda-approves-telixs-brain-cancer-imaging-drug-pixclara/"},{"label":"Joint EANM/EANO/RANO/SNMMI practice guidelines for PET imaging of gliomas with radiolabelled amino acids and FDG (2018)","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC6351513/"}],"tags":["amino acid PET","glioma","newly approved"],"related":["f-18-fdopa","f-18"],"indications":["glioblastoma"],"sections":[],"technologies":["pet","pet-ct"],"targets":[],"drugs":[],"companies":["telix"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Pixclara","modality":"PET tracer","mechanism":"An amino-acid analogue taken up by the L-type amino-acid transporters (LAT1/LAT2) that are upregulated on glioma cells, without being metabolically incorporated into protein. Because uptake tracks amino-acid transport rather than glucose metabolism, it gives much better contrast than FDG in the brain, where normal grey matter is a high glucose consumer but a low amino-acid transporter.","approvals":[{"region":"US","year":2026,"indication":"Use with PET to differentiate recurrent or progressive glioma from treatment-related change, in conjunction with other diagnostic evaluations, in adults and paediatric patients 1 month of age and older"}],"mechanismSteps":[],"dosing":{"route":"Intravenous bolus injection","schedule":"Adults: 185-259 MBq (5-7 mCi); paediatric patients 1 month and older: 3 MBq/kg (0.081 mCi/kg), minimum 14 MBq, maximum 259 MBq","source":"https://telixpharma.com/wp-content/uploads/2026/09/USPI_PIXCLARA_Sep2026.pdf"},"toxicity":[{"event":"Headache","anyGradePct":0.5,"source":"https://telixpharma.com/wp-content/uploads/2026/09/USPI_PIXCLARA_Sep2026.pdf"}],"access":[],"regulatoryEvents":[{"date":"2026-09-11","type":"approval","region":"US","note":"Pixclara, NDA 218592 (Telix Pharmaceuticals US), original approval; FDA classification Type 1 new molecular entity","source":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=218592"}]},{"id":"f-18-florquinitau","kind":"drug","name":"Florquinitau F-18","aka":["Tauklarify","florquinitau F 18 injection"],"tldr":"A new PET scan tracer, approved by the FDA in August 2026, that shows tangled tau protein in the brain of adults with memory or thinking problems who are being assessed for Alzheimer's disease. It is read alongside other tests: a negative scan does not rule tau out and a positive one does not prove it.","summary":"Tauklarify (florquinitau F 18 injection), sponsored by Cerveau (Lantheus), was approved by the FDA on 13 August 2026 under NDA 220496 (original approval, FDA classification Type 1 new molecular entity, standard review). It is indicated for PET of the brain in adults with cognitive impairment who are being evaluated for Alzheimer's disease, to identify patients with tau neurofibrillary tangle (NFT) pathology. The label limits use to Alzheimer's disease: safety and effectiveness are not established for non-Alzheimer tauopathies, and it warns that a negative scan does not exclude, and a positive scan does not confirm, tau NFT pathology.\n\nThe recommended activity is 185 MBq (5 mCi) as an intravenous bolus in up to 10 mL, with imaging started about 90 minutes after injection; the whole-body effective dose from 185 MBq in an adult is estimated at 5.4 mSv, before any CT. CYP1A2 inducers, including tobacco smoking, should be avoided for at least 7 days beforehand. Effectiveness rests on two blinded read studies (279 and 338 subjects) in which five independent readers per study classified scans as tau-positive or negative against a reference standard built from cognitive status and amyloid PET; in Study 1, positive percent agreement ranged from 80% to 88% across readers and negative percent agreement from 98% to 99%. Across 1,734 subjects in the clinical trials, the most common adverse reaction was headache (0.7%).","status":"approved","asOf":"2026-09-27","links":[{"label":"FDA label: Tauklarify (florquinitau F 18 injection), August 2026","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2026/220496Orig1s000lbl.pdf"},{"label":"Drugs@FDA: NDA 220496, Tauklarify","url":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=220496"},{"label":"FDA approval letter: NDA 220496, 13 August 2026","url":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2026/220496Orig1s000ltr.pdf"}],"tags":["tau PET","diagnostic","neurology","newly approved"],"related":["alzheimers-disease","f-18-flortaucipir","f-18-florbetapir","f-18-flutemetamol","f-18-florbetaben","f-18"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["lantheus"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Tauklarify","modality":"PET tracer","mechanism":"A fluorine-18 labelled tracer that binds aggregated tau protein (in-vitro dissociation constant 0.3 nM in post-mortem brain homogenates containing tau neurofibrillary tangles). It crosses the blood-brain barrier, so PET shows where tau tangles, one of the two lesions that define Alzheimer's disease pathologically, have built up.","approvals":[{"region":"US","year":2026,"indication":"PET of the brain in adults with cognitive impairment who are being evaluated for Alzheimer's disease, to identify patients with tau neurofibrillary tangle pathology"}],"mechanismSteps":[],"dosing":{"route":"Intravenous bolus","schedule":"185 MBq (5 mCi) in up to 10 mL; PET imaging starts approximately 90 minutes after injection","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2026/220496Orig1s000lbl.pdf"},"toxicity":[{"event":"Headache","anyGradePct":0.7,"source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2026/220496Orig1s000lbl.pdf"}],"access":[],"regulatoryEvents":[{"date":"2026-08-13","type":"approval","region":"US","note":"Tauklarify, NDA 220496 (Cerveau/Lantheus), original approval; FDA classification Type 1 new molecular entity, standard review","source":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=220496"}]},{"id":"f-18-flortaucipir","kind":"drug","name":"Flortaucipir F-18","aka":["Tauvid","18F-AV-1451","18F-T807"],"tldr":"A PET scan tracer that shows the tangled tau protein build-up in the brain seen in Alzheimer's disease, used alongside amyloid testing and clinical assessment, not on its own.","summary":"Flortaucipir F-18 (Tauvid, Eli Lilly, developed by Avid Radiopharmaceuticals) was approved by the FDA on 28 May 2020, the first tau PET tracer to reach the US market. It is indicated for PET imaging of the brain to estimate the density and distribution of aggregated tau neurofibrillary tangles in adult patients with cognitive impairment being evaluated for AD; the label explicitly states Tauvid is not indicated for evaluating chronic traumatic encephalopathy, since tau conformation and distribution differ in that condition. The EMA-approved indication (Tauvid EPAR) is PET imaging to assess the neocortical distribution of aggregated tau neurofibrillary tangles.\n\nThe recommended dose is 370 MBq (10 mCi) as an intravenous bolus in up to 10 mL, with a 20-minute PET image acquired starting about 80 minutes post-injection; the maximum mass dose is 20 micrograms and effective dose from 370 MBq is about 8.7 mSv. A positive scan (Braak-stage-like scoring, described in the label as 'B3' tau pathology, meaning widely distributed neocortical uptake in posterolateral temporal, occipital or parietal/precuneus regions with or without frontal involvement) supports a diagnosis of AD only in conjunction with clinical and other diagnostic evaluation; the EMA label also notes variable specificity and the possibility of false positives.\n\nIn the 2024 Alzheimer's Association revised diagnostic criteria, tau PET is treated as a 'Core 2' biomarker used to stage AD severity once amyloid positivity (Core 1) has established the diagnosis, rather than as a stand-alone diagnostic test. The 2025 SNMMI/Alzheimer's Association appropriate use criteria rate tau PET as 'appropriate' (score 8) alongside amyloid PET for determining eligibility for an approved amyloid-targeting therapy, though the workgroup notes that tau PET for treatment eligibility is not itself required in the FDA prescribing information for lecanemab or donanemab. There is no dedicated Medicare national coverage determination for tau PET; it falls under the same PET framework applied by CMS and local Medicare Administrative Contractors as other diagnostic radiopharmaceuticals.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Tauvid (flortaucipir F 18 injection)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/212123s031lbl.pdf"},{"label":"EMA EPAR product information: Tauvid","url":"https://www.ema.europa.eu/en/documents/product-information/tauvid-epar-product-information_en.pdf"},{"label":"SNMMI/Alzheimer's Association: updated appropriate use criteria for amyloid and tau PET (2025)","url":"https://jnm.snmjournals.org/content/early/2025/01/07/jnumed.124.268756"},{"label":"PMC review: Tauvid, the first FDA-approved PET tracer for imaging tau pathology","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC7911942/"}],"tags":["tau PET","diagnostic","neurology"],"related":["alzheimers-disease","f-18-florbetapir","f-18-flutemetamol","f-18-florbetaben","eli-lilly","f-18"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Tauvid","modality":"PET tracer","mechanism":"A fluorine-18 labelled tracer that binds paired helical filament tau, the aggregated, phosphorylated form of tau protein found in neurofibrillary tangles, allowing PET visualisation of the density and spatial spread of tau pathology.","approvals":[{"region":"US","year":2020,"indication":"PET imaging of the brain to estimate density and distribution of aggregated tau neurofibrillary tangles in adults with cognitive impairment being evaluated for Alzheimer's disease"}],"mechanismSteps":[],"dosing":{"route":"Intravenous bolus","schedule":"370 MBq (10 mCi) single dose in up to 10 mL; 20-minute PET image starting approximately 80 minutes after injection","monitoring":"Visual scoring of neocortical tau pattern distribution (B1-B3 Braak-like staging); used alongside amyloid PET/CSF as a Core 2 staging biomarker","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/212123s031lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"flotufolastat","kind":"drug","name":"Flotufolastat F-18","aka":[],"tldr":"Flotufolastat is a third PSMA PET tracer, with a radiohybrid chemistry designed to be reused for therapy.","summary":"Flotufolastat F-18 (Posluma) is a radiohybrid PSMA ligand: a silicon-fluoride acceptor allows 18F labelling for PET while the same scaffold can carry 177Lu for therapy, so imaging and treatment agents share one chemistry. It is used for PSMA PET in men with prostate cancer at initial staging and at biochemical recurrence. The LIGHTHOUSE (initial staging) and SPOTLIGHT (biochemical recurrence) trials supported approval in May 2023. Low urinary excretion aids reading of the pelvis, where bladder activity can obscure local recurrence with other tracers. It is the third PSMA PET tracer in the US after gallium-68 PSMA-11 and Pylarify, and head-to-head comparisons are limited. For a newcomer, it is a PSMA scan agent designed from the start to be reused for therapy.","status":"approved","asOf":"2026-09-06","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Flotufolastat%20F-18"}],"tags":[],"related":["f-18","ga-68","lu-177"],"indications":["prostate"],"sections":[],"technologies":["psma-pet"],"targets":["psma"],"drugs":[],"companies":["blue-earth-diagnostics"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Posluma","code":"18F-rhPSMA-7.3","modality":"PET imaging agent","mechanism":"Radiohybrid PSMA ligand; silicon-fluoride acceptor allows 18F imaging and 177Lu therapy on the same scaffold.","approvals":[{"region":"US","year":2023,"indication":"PSMA PET in prostate cancer"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"fluciclovine-f18","kind":"drug","name":"Fluciclovine F-18","aka":[],"tldr":"Fluciclovine F-18 was the first PET tracer approved for finding recurrent prostate cancer after treatment (2016), and has been largely superseded since 2020 by PSMA PET.","summary":"Approved May 2016 for suspected recurrence with rising PSA; detection ~68% overall, lower at low PSA. EMSPOT/EMPIRE-1 (Lancet 2021) showed fluciclovine-guided salvage radiotherapy improved failure-free survival. PSMA PET (Ga-68 PSMA-11, piflufolastat, flotufolastat) has higher detection and displaced it.","status":"approved","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Fluciclovine_(18F)","links":[{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Axumin"}],"tags":["gap-fill","diagnostic"],"related":["f-18","ga-68"],"indications":["prostate","glioblastoma"],"sections":[],"technologies":["pet","pet-ct"],"targets":[],"drugs":[],"companies":["blue-earth-diagnostics"],"institutions":[],"pathways":[],"terms":["biochemical-recurrence"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Axumin","modality":"PET radiotracer (synthetic amino acid)","mechanism":"18F-labelled leucine analogue taken up via LAT1/ASCT2 amino-acid transporters upregulated in prostate cancer; low urinary excretion improves pelvic imaging.","approvals":[{"region":"US","year":2016,"indication":"PET imaging in men with suspected prostate cancer recurrence based on elevated PSA"},{"region":"EU","year":2017,"indication":"Same"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"f-18-fdg-brain","kind":"drug","name":"Fludeoxyglucose F-18 (brain metabolism)","aka":["FDG-PET brain","18F-FDG"],"tldr":"The standard PET tracer for measuring how the brain is using energy; a pattern of low activity in particular brain regions can help doctors work out which type of dementia a patient has.","summary":"Fludeoxyglucose F-18 (FDG) is the general-purpose PET metabolic tracer used across oncology, cardiology and neurology; it is not brain-specific as a product, but brain FDG PET is a distinct, well-established clinical application. Reduced glucose metabolism follows a regional pattern that differs by disease: temporoparietal and posterior cingulate hypometabolism is typical of Alzheimer's disease, while frontal and/or anterior temporal hypometabolism points to frontotemporal dementia, and this pattern difference is the main clinical use of FDG-PET in cognitive impairment.\n\nIn the United States, Medicare's national coverage determination for FDG-PET in dementia (NCD 220.6.13) covers a scan specifically to help differentiate Alzheimer's disease from frontotemporal dementia, in patients with a recent dementia diagnosis and at least 6 months of documented cognitive decline whose presentation leaves this distinction clinically uncertain after a comprehensive specialist evaluation; a prior brain SPECT or FDG-PET scan for the same question generally precludes a repeat scan within a year. All other dementia uses of FDG-PET (for example distinguishing other neurodegenerative diseases, or use outside a CMS-approved clinical trial in mild cognitive impairment) remain nationally non-covered under this determination, a materially narrower coverage pathway than the one now in force for amyloid PET.\n\nFDG-PET brain imaging does not require thyroid blockade or specialised handling beyond standard F-18 PET radiopharmacy practice, and dosing follows general oncologic/neurologic FDG protocols (typically around 185-370 MBq IV, imaging beginning about 30-45 minutes later, with the patient resting quietly in a darkened, low-stimulation room during uptake to standardise regional brain activity). Because FDG uptake reflects neuronal activity rather than a specific pathological protein, it complements rather than replaces amyloid and tau PET: FDG shows the functional consequence of neurodegeneration, while amyloid and tau tracers show the underlying molecular pathology.","status":"approved","asOf":"2026-09-22","links":[{"label":"CMS NCD 220.6.13: FDG PET for Dementia and Neurodegenerative Diseases","url":"https://www.cms.gov/regulations-and-guidance/guidance/transmittals/downloads/r24ncd.pdf"},{"label":"CMS coding article: PET scan coverage reference table including FDG dementia indication (A53134)","url":"https://www.cms.gov/medicare-coverage-database/view/article.aspx?articleId=53134"}],"tags":["FDG PET","diagnostic","neurology","metabolic imaging"],"related":["alzheimers-disease","fludeoxyglucose-f18","fdg-pet","tc-99m-hmpao-brain","f-18"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"A glucose analogue labelled with fluorine-18 that is taken up by cells in proportion to glucose metabolism and trapped after phosphorylation; in the brain, regional FDG uptake reflects synaptic activity, so characteristic patterns of reduced metabolism can distinguish different neurodegenerative diseases.","approvals":[{"region":"US","year":2004,"indication":"FDG-PET nationally covered by Medicare specifically to differentiate Alzheimer's disease from frontotemporal dementia in patients with an uncertain diagnosis after comprehensive specialist evaluation (NCD 220.6.13)"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"Typical adult brain FDG-PET protocol: ~185-370 MBq IV, patient rested in a quiet, dimly lit room during the ~30-45 minute uptake phase, then PET imaging","monitoring":"Visual and statistical/voxel-based comparison of regional glucose metabolism against normative databases to identify disease-specific hypometabolism patterns","source":"https://www.cms.gov/regulations-and-guidance/guidance/transmittals/downloads/r24ncd.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"fludeoxyglucose-f18","kind":"drug","name":"Fludeoxyglucose F-18 (FDG)","aka":[],"tldr":"The radioactive sugar used in almost every cancer PET scan, approved in the 1990s and made fresh each day by regional cyclotrons.","summary":"Fludeoxyglucose F-18 was the first PET radiopharmaceutical approved by the FDA (1994, initially for epilepsy foci and cardiac viability) and gained its oncology indication in 2000 for assessing abnormal glucose metabolism to assist in evaluating malignancy in patients with known or suspected cancer. It is produced under multiple abbreviated NDAs by commercial and academic cyclotron networks (PETNET, Cardinal Health, SOFIE, hospital sites) and is the tracer behind staging, response assessment (Deauville in lymphoma, PERCIST) and surveillance across most solid tumours. Its weaknesses, uptake in inflammation and poor sensitivity for indolent or low-glucose tumours, drive the development of target-specific tracers.","status":"approved","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Fludeoxyglucose_(18F)","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Fludeoxyglucose%20F%2018"}],"tags":["test"],"related":["f-18"],"indications":["nsclc"],"sections":[],"technologies":["fdg-pet","pet-ct","pet"],"targets":[],"drugs":[],"companies":["petnet-solutions","cardinal-health","sofie-biosciences"],"institutions":[],"pathways":[],"terms":["suv"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["What a result means: 'hot spots' show tissue burning glucose fast; in a person with cancer they usually mark tumour, but infection, healing and brown fat can light up too, so findings are interpreted with CT and biopsy."],"brand":"FDG (multiple manufacturers)","modality":"PET imaging agent (glucose analogue)","mechanism":"18F-labelled glucose analogue taken up through GLUT transporters and trapped after phosphorylation by hexokinase, so metabolically active tumours accumulate signal.","approvals":[{"region":"US","year":1994,"indication":"First FDG NDA (neurology and cardiology indications)"},{"region":"US","year":2000,"indication":"Oncology: assessment of abnormal glucose metabolism to assist in evaluating malignancy"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"f-18-fdopa","kind":"drug","name":"Fluorodopa F-18","aka":["18F-FDOPA","6-[18F]fluoro-L-DOPA","Fluorodopa F 18 Injection"],"tldr":"A tracer originally built to look at brain dopamine cells in suspected Parkinson's disease. Because certain hormone-producing tumours use the same chemical machinery, doctors also use it, off-label, to find those tumours -- especially adrenal gland tumours called pheochromocytoma.","summary":"Fluorodopa F 18 Injection was approved by FDA in 2019 (NDA 200655, sponsor The Feinstein Institutes for Medical Research) solely for PET imaging of dopaminergic nerve terminals in adults with suspected Parkinsonian syndromes; that is a neurological indication, not an oncological one, and it is the only indication on the US label. The recommended dose is 185 MBq (5 mCi) IV.\n\nIn oncology, 18F-FDOPA is used off-label, but with strong evidence and explicit guideline support: the 2019 EANM/SNMMI procedure standard for phaeochromocytoma and paraganglioma names 18F-FDOPA (alongside 123I-MIBG) as a first-line tracer, ahead of 68Ga-DOTATATE and 18F-FDG. In a prospective head-to-head study of 97 patients, FDOPA detected all 55 confirmed pheochromocytomas versus 25 of 55 for 68Ga-DOTATOC (sensitivity 100% vs 49%, p<0.0001), though DOTATATE-family tracers retain an edge for extra-adrenal and SDHx-related metastatic disease. FDOPA is also used, again off-label, in brain tumour imaging (glioma grading and recurrence, alongside FET) under joint EANM/EANO/RANO/SNMMI amino-acid PET guidelines.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Fluorodopa F 18 Injection","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/200655s000lbl.pdf"},{"label":"Prospective comparison of 18F-FDOPA and 68Ga-DOTATOC PET/CT in pheochromocytoma/paraganglioma (2023)","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC10728412/"},{"label":"EANM/SNMMI 2019 practice guideline for radionuclide imaging of phaeochromocytoma and paraganglioma","url":"https://snmmi.org/common/Uploaded%20files/Web/Clinical%20Practice/Procedure%20Standards/2019/EANM%20SNMMI%20guideline%20on%20radionuclide%20imaging%20of%20phaeochromocytoma%20and%20paraganglioma.pdf"}],"tags":["amino acid PET","off-label oncology use","PPGL"],"related":["cu-64-dotatate","ga-68-dotatoc","i-123-mibg","f-18-fet","f-18","ga-68","i-123"],"indications":["pheochromocytoma-paraganglioma","metastatic-ppgl","neuroendocrine","glioblastoma"],"sections":[],"technologies":["pet","pet-ct"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"A fluorinated analogue of L-DOPA that is taken up by the amino-acid transport system and converted by aromatic L-amino-acid decarboxylase (AADC) into a trapped dopamine analogue. Dopaminergic neurons take it up for the FDA-approved neurological indication; the same AADC pathway is highly active in cells of neural-crest and neuroendocrine origin, which is why the tracer also concentrates strongly in pheochromocytoma, paraganglioma and other well-differentiated neuroendocrine tumours.","approvals":[{"region":"US","year":2019,"indication":"PET imaging to visualise dopaminergic nerve terminals in the striatum in adults with suspected Parkinsonian syndromes (neurological indication; oncology use is off-label)"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection over 1 minute","schedule":"185 MBq (5 mCi) in adults","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/200655s000lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"fluoroestradiol-f18","kind":"drug","name":"Fluoroestradiol F-18 (FES PET)","aka":[],"tldr":"A PET scan that shows which breast cancer deposits still have oestrogen receptors, helping decide whether hormone therapy will work when biopsy is impractical.","summary":"Fluoroestradiol F-18 is a PET radiotracer in which 18F-labelled oestradiol binds oestrogen receptor alpha, imaging ER expression across every lesion in the body in a single non-invasive scan. It was approved in the US in May 2020 as an adjunct to biopsy for detecting ER-positive lesions in recurrent or metastatic breast cancer, and entered NCCN guidelines in 2024. It is used when biopsy is impractical or when lesions may have lost ER, because it predicts endocrine responsiveness and reveals heterogeneous receptor loss that a single biopsy would miss. It also serves as a pharmacodynamic tool in trials of ER degraders, measuring receptor occupancy, and is under study in ER-positive ovarian and endometrial cancers. Uptake in the liver limits assessment of hepatic metastases. FES PET tells the oncologist whether hormone therapy still has a target.","status":"approved","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Fluoroestradiol_F-18","links":[{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Cerianna"}],"tags":["gap-fill","diagnostic"],"related":["f-18"],"indications":[],"sections":[],"technologies":["pet","pet-ct"],"targets":[],"drugs":[],"companies":["ge-healthcare"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Cerianna","modality":"PET radiotracer (oestrogen receptor ligand)","mechanism":"18F-labelled oestradiol binds oestrogen receptor alpha, imaging ER expression across all lesions non-invasively.","approvals":[{"region":"US","year":2020,"indication":"Detection of ER-positive lesions as an adjunct to biopsy in patients with recurrent or metastatic breast cancer"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"f-18-fluorothymidine","kind":"drug","name":"Fluorothymidine F-18 (FLT)","aka":["18F-FLT","3'-deoxy-3'-[18F]fluorothymidine"],"tldr":"An experimental PET tracer that measures how fast tumour cells are dividing, rather than how much sugar they burn. It has been studied in research settings for over 20 years but has never been approved as a medicine.","summary":"18F-FLT has been an investigational PET agent since it was first reported in 1998, and remains one so today: it is supplied only under Investigational New Drug (IND) exemptions or Radioactive Drug Research Committee (RDRC)-approved basic science protocols, and no marketing application has been filed anywhere. The US National Cancer Institute's Cancer Imaging Program holds a centralised, multi-source IND that lets academic sites use FLT made by any of several suppliers with a Drug Master File on record, which has supported dozens of single- and multi-centre trials, mostly in breast, lung and brain cancer, evaluating early response to chemotherapy.\n\nFLT's main limitation is that its signal is diluted by TK1 activity in normal proliferating tissue -- bone marrow and liver in particular -- giving high background uptake that can obscure metastases in those organs, and its plasma level is affected by co-administered chemotherapy and some pain medications via hepatic glucuronidation. Studies correlate FLT uptake with the Ki-67 proliferation marker in breast, lung and brain tumours, and FLT-PET has shown early, quantifiable drops in uptake after starting chemotherapy, but larger controlled trials with survival endpoints have not been completed, and no clinical guideline currently recommends it outside a trial setting.","status":"phase-2","asOf":"2026-09-22","links":[{"label":"NCI Investigator's Brochure: [F-18]FLT, an investigational PET radiopharmaceutical","url":"https://dctd.cancer.gov/drug-discovery-development/reagents-materials/imaging-ind-resources/documentation/flt-ib.pdf"},{"label":"Applications of PET imaging with the proliferation marker 18F-FLT (review, 2015)","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC4415691/"},{"label":"SNMMI PET Center of Excellence FLT factsheet","url":"https://snmmi.org/common/Uploaded%20files/Web/Centers/PET%20Center%20of%20Excellence/FLT_07-11-12%20Final.pdf"}],"tags":["proliferation imaging","investigational","TK1"],"related":["f-18"],"indications":["breast-her2-positive","glioblastoma","nsclc"],"sections":[],"technologies":["pet"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"A thymidine analogue that is taken up and phosphorylated by thymidine kinase 1 (TK1) during the S-phase of the cell cycle, then trapped intracellularly because the phosphorylated form cannot cross the cell membrane back out. Because TK1 activity tracks DNA synthesis, FLT uptake is a direct measure of cellular proliferation rather than glucose metabolism (which 18F-FDG measures) -- in principle a closer PET analogue of the Ki-67 proliferation index measured on biopsy.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"f-18-flurpiridaz","kind":"drug","name":"Flurpiridaz F-18","aka":["18F-flurpiridaz","BMS-747158-02"],"tldr":"The newest heart PET tracer, approved in the US in September 2024. It sticks tightly to a protein inside heart-muscle mitochondria in proportion to blood flow, lasts long enough to be made off site and shipped like a hospital's regular PET drug, and is the first cardiac PET tracer practical to pair with a treadmill exercise test.","summary":"Flyrcado (flurpiridaz F-18) is a fluorine-18 mitochondrial complex I-binding PET myocardial perfusion agent approved by the FDA on 27 September 2024 (NDA 215168, GE HealthCare), the first new PET MPI agent approved in the US in over a decade and the first cardiac PET tracer with a half-life practical for exercise stress protocols. Its mechanism, high-affinity binding to complex I rather than ion-pump uptake, gives a first-pass extraction fraction of about 94%, markedly higher and flatter across flow rates than sestamibi (55-68%), tetrofosmin (54%) or Rb-82 (roughly 40-70%), which its sponsor and independent reviews report translates into sharper contrast for smaller or milder perfusion defects.\n\nThe approved indication is PET myocardial perfusion imaging under rest or stress (pharmacologic or exercise) in adult patients with known or suspected coronary artery disease, to evaluate for myocardial ischaemia and infarction. Because F-18's 110-minute half-life is roughly ten times that of Rb-82 and eleven times N-13 ammonia's, Flyrcado can be manufactured off site and delivered as a ready-to-use unit dose like FDG, potentially widening PET MPI access beyond centres with an on-site generator or cyclotron, including for patients who are difficult to image by SPECT (high body-mass index, women with breast attenuation artefact).\n\nMost common adverse reactions in the pivotal programme (occurring in at least 2% of subjects across rest and stress imaging) were dyspnoea, headache, angina pectoris, chest pain, fatigue, ST-segment changes, flushing, nausea, abdominal pain, dizziness and arrhythmia. As a newly approved agent, real-world comparative outcome and cost-effectiveness data against SPECT and existing PET tracers are still accumulating.","asOf":"2026-09-22","links":[{"label":"FDA approval letter and package, NDA 215168 (Flyrcado)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2024/215168Orig1s000Approv.pdf"},{"label":"FDA label: Flyrcado (flurpiridaz F 18) injection, September 2024","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/215168s000lbl.pdf"},{"label":"FDA news release: FDA approves imaging drug for evaluation of myocardial ischemia and infarction (27 September 2024)","url":"https://www.fda.gov/drugs/news-events-human-drugs/fda-approves-imaging-drug-evaluation-myocardial-ischemia-and-infarction"},{"label":"SNMMI/JNM procedure standard: 18F-flurpiridaz PET myocardial perfusion imaging and blood flow quantification","url":"https://snmmi.org/common/Uploaded%20files/Web/Clinical%20Practice/Procedure%20Standards/2025/Flurpiridaz%20Procedure%20Standard-JNM.pdf"}],"tags":["PET","myocardial perfusion","mitochondrial complex I"],"related":["rb-82-chloride","n-13-ammonia","tc-99m-sestamibi","f-18","n-13","rb-82"],"indications":["coronary-artery-disease"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["ge-healthcare"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Flyrcado","modality":"PET tracer","mechanism":"Flurpiridaz F-18 is a fluorinated structural analogue of pyridaben, an insecticidal inhibitor of mitochondrial complex I (NADH:ubiquinone oxidoreductase). It binds with high affinity to complex I in cardiomyocyte mitochondria without impairing viability, giving a very high and largely flow-independent first-pass myocardial extraction fraction (reported at approximately 94% in preclinical and kinetic modelling studies) and slow washout, so uptake tracks blood flow more linearly across a wider flow range than the older SPECT or Rb-82 agents, with less roll-off at high flow. Its 110-minute F-18 half-life, more than ten times longer than Rb-82 or N-13 ammonia, allows off-site cyclotron production and unit-dose distribution like FDG, and is long enough to support exercise stress imaging, which is impractical with the shorter-lived PET perfusion tracers.","approvals":[{"region":"US","year":2024,"indication":"PET myocardial perfusion imaging (MPI) under rest or stress (pharmacologic or exercise) in adult patients with known or suspected coronary artery disease, to evaluate for myocardial ischaemia and infarction"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"Per FDA label dosing tables for rest and stress imaging (pharmacologic or exercise stress); supplied at 190-2,050 MBq/mL (5-55 mCi/mL) at end of synthesis","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/215168s000lbl.pdf"},"toxicity":[{"event":"Dyspnoea, headache, angina pectoris, chest pain, fatigue, ST-segment changes, flushing, nausea, abdominal pain, dizziness, arrhythmia (most common, combined rest and stress imaging)","source":"https://www.fda.gov/drugs/news-events-human-drugs/fda-approves-imaging-drug-evaluation-myocardial-ischemia-and-infarction"}],"access":[],"regulatoryEvents":[{"date":"2024-09-27","type":"approval","region":"US","note":"FDA approved Flyrcado (flurpiridaz F 18) injection, NDA 215168, for PET myocardial perfusion imaging under rest or stress (pharmacologic or exercise) in adults with known or suspected CAD.","source":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2024/215168Orig1s000Approv.pdf"}]},{"id":"f-18-flutemetamol","kind":"drug","name":"Flutemetamol F-18","aka":["Vizamyl"],"tldr":"A PET scan tracer used to check whether a patient's brain has amyloid plaques, the hallmark of Alzheimer's disease, and whether they can be treated with amyloid-lowering drugs.","summary":"Flutemetamol F-18 (Vizamyl, GE HealthCare) was FDA-approved in October 2013 for PET imaging of the brain to estimate beta-amyloid neuritic plaque density in adults with cognitive impairment being evaluated for AD and other causes of cognitive decline. As with the other amyloid tracers, the US label was updated (current version dated 2025/2026) to add a second indication, selection of patients indicated for amyloid beta-directed therapy, alongside the diagnostic indication. The EMA-approved indication (EPAR, EU) is imaging to help diagnose Alzheimer's disease and other causes of memory loss.\n\nThe recommended dose is 185 MBq (5 mCi) given as an intravenous bolus over 40 seconds in up to 10 mL, maximum mass dose 20 micrograms, with 10 to 20-minute PET images acquired 60 to 120 minutes after injection; the resulting effective dose is about 5.9 mSv (32 microSv/MBq). Vizamyl is contraindicated in patients with known hypersensitivity to polysorbate 80, an excipient, which is a distinguishing safety point versus the other amyloid tracers.\n\nInterpretation is by visual assessment of grey-white matter contrast (a positive scan shows loss of the normal grey-white distinction from cortical tracer retention), and flutemetamol has a validated tracer-specific linear conversion to the Centiloid scale, allowing quantitative reporting alongside the qualitative read. In the US, amyloid PET coverage for Medicare beneficiaries, including flutemetamol scans, follows the post-2023 framework in which CMS retired the national coverage determination and left individual coverage decisions to local Medicare Administrative Contractors, removing the former one-scan-per-lifetime limit.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Vizamyl (flutemetamol F 18 injection)","url":"https://dailymed.nlm.nih.gov/dailymed/getFile.cfm?setid=b3558f16-8f9a-4e55-8d9c-836427ebaa57&type=pdf"},{"label":"EMA EPAR product information: Vizamyl","url":"https://www.ema.europa.eu/en/documents/product-information/vizamyl-epar-product-information_en.pdf"},{"label":"Zhang et al.: Centiloid scaling for quantification of brain amyloid with [18F]flutemetamol","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC6281542/"},{"label":"CMS: decision memo removing the amyloid PET national coverage determination (NCA-CAL 308)","url":"https://www.cms.gov/medicare-coverage-database/view/ncacal-decision-memo.aspx?proposed=N&ncaid=308"}],"tags":["amyloid PET","diagnostic","neurology"],"related":["alzheimers-disease","f-18-florbetapir","f-18-florbetaben","ge-healthcare","f-18"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Vizamyl","modality":"PET tracer","mechanism":"A fluorine-18 labelled benzothiazole derivative, structurally related to Pittsburgh Compound-B, that binds fibrillar beta-amyloid plaques for PET detection of cortical amyloid burden.","approvals":[{"region":"US","year":2013,"indication":"PET imaging of the brain to estimate beta-amyloid neuritic plaque density in adults with cognitive impairment being evaluated for AD and other causes of cognitive decline"},{"region":"US","year":2025,"indication":"Label update adding selection of patients indicated for amyloid beta-directed therapy"},{"region":"EU","year":2014,"indication":"Diagnostic use to help diagnose Alzheimer's disease and other causes of memory loss"}],"mechanismSteps":[],"dosing":{"route":"Intravenous bolus","schedule":"185 MBq (5 mCi) single dose within 40 seconds, in up to 10 mL, flushed with 5-15 mL saline; PET imaging 60-120 minutes after injection","monitoring":"Visual read of cortical grey-white contrast; Centiloid quantification available as an adjunct using a validated tracer-specific conversion equation","source":"https://dailymed.nlm.nih.gov/dailymed/getFile.cfm?setid=b3558f16-8f9a-4e55-8d9c-836427ebaa57&type=pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"fpi-2265","kind":"drug","name":"FPI-2265","aka":["Ac225-PSMA I&T"],"tldr":"FPI-2265 is an experimental radioligand therapy from Fusion Pharmaceuticals in phase 2 trials for prostate cancer, aimed at PSMA.","summary":"FPI-2265 is a radioligand therapy developed by Fusion Pharmaceuticals. Its target is PSMA (the sponsor names PSMA). The sponsor states: A PSMA-targeting ligand (PSMA-I&T) radiolabeled with the alpha-emitter actinium-225, delivering targeted alpha radiotherapy to PSMA-positive prostate cancer cells. ClinicalTrials.gov describes the intervention as: Small molecule capable of binding to the domain of PSMA radiolabeled with Ac225. It is the investigational product in 3 recruiting or active industry-led phase 2 and phase 3 interventional cancer trials, in prostate cancer. The largest, NCT05219500, plans to enrol 115 participants with primary completion was scheduled for 2025-05-30 on the registry. Status reflects the highest phase registered on ClinicalTrials.gov; no efficacy results are recorded here.","status":"phase-2","asOf":"2026-09-11","links":[{"label":"ClinicalTrials.gov: trials of FPI-2265","url":"https://clinicaltrials.gov/search?intr=FPI-2265"}],"tags":["pipeline","ctgov-ingest"],"related":["ac-225"],"indications":["prostate"],"sections":[],"technologies":[],"targets":["psma"],"drugs":[],"companies":["astrazeneca"],"institutions":[],"pathways":[],"terms":[],"trials":["nct07611110","nct05219500","nct07590934","nct06909825"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2 + sponsor pipeline pages)","editedOn":"2026-09-11"},"modality":"radioligand","mechanism":"A PSMA-targeting ligand (PSMA-I&T) radiolabeled with the alpha-emitter actinium-225, delivering targeted alpha radiotherapy to PSMA-positive prostate cancer cells.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ga-67-citrate","kind":"drug","name":"Gallium citrate Ga-67","aka":["67Ga-citrate","Gallium Citrate Ga 67"],"tldr":"One of the oldest cancer-imaging scans still on the market: an injectable form of radioactive gallium that collects in lymphomas and some other tumours (and in infections), imaged one to five days later. It has mostly been replaced by FDG-PET but is still FDA-approved and occasionally used.","summary":"Gallium Citrate Ga 67 Injection has held FDA approval since the 1970s (NDA 017478) for demonstrating the presence and extent of Hodgkin's disease, other lymphomas and bronchogenic carcinoma, and as an aid in detecting some acute inflammatory lesions; it is currently labelled and marketed by Curium. The adult dose is 74-185 MBq (2-5 mCi) IV, with optimal images typically obtained 48 hours post-injection, though acceptable images can be acquired anywhere from 6 to 120 hours afterward given considerable inter-patient biological variability.\n\nThe label itself flags the tracer's major limitation: up to 40% false-negative rates in some pathological conditions, an inability to distinguish tumour from acute inflammation without additional studies, and poor performance in lymphocytic lymphoma specifically, which the label states is not recommended for gallium imaging. FDG-PET has substantially displaced Ga-67 citrate for lymphoma staging and for fever-of-unknown-origin workups because it offers same-day imaging, higher spatial resolution and better sensitivity; gallium scintigraphy's most durable remaining niche is spinal and musculoskeletal infection imaging (often as SPECT/CT) in settings where FDG-PET is unavailable.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Gallium Citrate Ga-67 Injection (DailyMed, Curium US LLC)","url":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5f670c12-cca5-4d73-8a88-241f753d1bc7"}],"tags":["legacy agent","lymphoma imaging","SPECT"],"related":["ga-67"],"indications":[],"sections":[],"technologies":["spect","spect-ct"],"targets":[],"drugs":[],"companies":["curium"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"SPECT tracer","mechanism":"Free gallium ion, delivered as the citrate salt, is thought to accumulate in lysosomes and bind a soluble intracellular protein in certain viable tumours and in focal sites of infection or inflammation; the exact mechanism has never been fully characterised despite the tracer's decades of clinical use. Gallium-67 decays by electron capture with several gamma photopeaks, requiring a medium-energy collimator and triple-energy-window acquisition.","approvals":[{"region":"US","year":1976,"indication":"Demonstrating the presence and extent of Hodgkin's disease, lymphoma and bronchogenic carcinoma; aid in detecting some acute inflammatory lesions"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"74-185 MBq (2-5 mCi) in an average 70 kg adult; optimal imaging around 48 hours post-injection, acceptable from 6-120 hours","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=5f670c12-cca5-4d73-8a88-241f753d1bc7"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ga68-dotatate","kind":"drug","name":"Gallium-68 DOTATATE (and Cu-64 DOTATATE)","aka":[],"tldr":"The PET scan for neuroendocrine tumours that finds far more disease than older scans and confirms eligibility for lutetium radioligand therapy (the theranostic pair).","summary":"Ga-68 DOTATATE (Netspot, kit) approved June 2016; Cu-64 DOTATATE (Detectnet, 12.7-hour half-life allows central production) approved September 2020; Ga-68 DOTATOC (2019, academic). Changes management in about a third of patients; required before Lu-177 DOTATATE (Lutathera). Also images meningioma and paraganglioma.","status":"approved","asOf":"2026-09-08","links":[{"label":"Label: Netspot (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Netspot"},{"label":"Label: Detectnet (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Detectnet"}],"tags":["gap-fill","diagnostic"],"related":["ga-68","cu-64","lu-177"],"indications":["neuroendocrine","small-intestinal-net","pancreatic-net","lung-net"],"sections":[],"technologies":["sstr-pet","pet-ct","prrt","radioligand-therapy"],"targets":["sstr2"],"drugs":[],"companies":["novartis","curium"],"institutions":[],"pathways":[],"terms":["theranostics","prrt-term"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Netspot / Detectnet","modality":"PET radiotracer (somatostatin receptor ligand)","mechanism":"Radiolabelled somatostatin analogue binding SSTR2 on neuroendocrine tumours; PET replaces the older In-111 octreotide SPECT with higher sensitivity and same-day imaging.","approvals":[{"region":"US","year":2016,"indication":"PET localisation of SSTR-positive neuroendocrine tumours (Ga-68 DOTATATE)"},{"region":"US","year":2020,"indication":"Same (Cu-64 DOTATATE)"},{"region":"EU","year":2017,"indication":"SomaKit TOC (Ga-68 DOTATOC)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ga-68-dotatoc","kind":"drug","name":"Gallium-68 edotreotide (DOTATOC)","aka":["68Ga-DOTATOC","Ga 68 DOTATOC Injection","Edotreotide"],"tldr":"A cousin of the Ga-68 DOTATATE and Cu-64 DOTATATE scans: it sticks to the same receptor on neuroendocrine tumours and lets PET find them. It is FDA-approved but, unusually, has no brand name and no pharmaceutical-company sponsor.","summary":"Ga 68 DOTATOC Injection was approved by FDA on 21 August 2019 under NDA 210828, an unusual academic new drug application held by the University of Iowa Health Care PET Imaging Center rather than a company. Approval covered PET localisation of somatostatin receptor-positive neuroendocrine tumours in adult and paediatric patients, based on a retrospective analysis of three prospective trials plus a literature meta-analysis; no deaths or serious adverse events were reported among the 334 patients reviewed for the pivotal readout. In the EU, the equivalent product is licensed as SomaKit TOC (December 2016).\n\nThe adult dose is 148 MBq (4 mCi), with a paediatric weight-based dose of 1.59 MBq/kg (minimum 11.1 MBq, maximum 111 MBq). Because it has no proprietary name, it is often described in the literature simply as 68Ga-DOTATOC. In direct comparisons, 68Ga-DOTATOC and 64Cu-DOTATATE perform similarly, while 18F-FDOPA has shown superior sensitivity for pheochromocytoma specifically. The therapeutic counterpart of the same peptide, 177Lu-edotreotide (ITM-11), remains unapproved in the US as of September 2026 after a complete response letter over manufacturing issues.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA approval letter, NDA 210828, Ga-68-DOTATOC (2019)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210828Orig1s000Approv.pdf"},{"label":"FDA multi-discipline review, NDA 210828","url":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210828Orig1s000MultidisciplineR.pdf"},{"label":"Sunderland & Graham, J Nucl Med 2020: an academic medical centre's journey through the FDA NDA process for 68Ga-DOTATOC","url":"https://jnm.snmjournals.org/content/jnumed/early/2020/02/06/jnumed.119.238287.full.pdf"}],"tags":["SSTR2","NET imaging","academic NDA"],"related":["cu-64-dotatate","ga68-dotatate","itm-11","f-18","ga-68","cu-64","lu-177"],"indications":["neuroendocrine","pancreatic-net","small-intestinal-net"],"sections":[],"technologies":["sstr-pet","pet-ct"],"targets":["sstr2"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"A somatostatin analogue peptide (octreotide backbone with a DOTA chelator) that binds somatostatin receptor subtype 2, the same receptor targeted by DOTATATE. DOTATOC has somewhat higher affinity for SSTR5 than DOTATATE, which can matter for a minority of tumours, but the two peptides are broadly interchangeable in practice.","approvals":[{"region":"US","year":2019,"indication":"PET localisation of somatostatin receptor-positive neuroendocrine tumours in adult and paediatric patients"},{"region":"EU","year":2016,"indication":"PET localisation of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumours (as SomaKit TOC)"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"Adults: 148 MBq (4 mCi), range 111-185 MBq; paediatric: 1.59 MBq/kg, minimum 11.1 MBq, maximum 111 MBq","source":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/210828Orig1s000MultidisciplineR.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ga-68-fapi-46","kind":"drug","name":"Gallium-68 FAPI-46","aka":["68Ga-FAPI-46","Ga-68 FAPi-46"],"tldr":"An experimental PET tracer that lights up the scaffolding cells cancers build around themselves, not the cancer cells directly. It is still being tested, not yet an approved medicine.","summary":"68Ga-FAPI-46 is one of the most advanced compounds in the FAPI family under joint development by SOFIE Biosciences and GE HealthCare (global licence signed 2024). It has been studied prospectively in several hundred patients across breast, colorectal, pancreatic, head and neck, and other solid tumours. In a single-centre phase 2 trial at University Hospital Essen (NCT05160051, 155 patients scanned, reported in Lancet Oncology 2025), the tracer's positive predictive value for detecting immunohistochemically FAP-positive tumours was 90% on a per-patient basis and 92% per region, meeting the trial's pre-specified threshold.\n\nSeparate US phase 2 studies are running in resectable or borderline-resectable pancreatic ductal adenocarcinoma (NCT05262855/NCT05518903) across Mayo Clinic, UCLA, NYU Langone and BAMF Health, comparing FAPI-46 PET detection of cancer-associated fibroblasts against surgical histopathology, with phase 3 planning under way as of mid-2024. The tracer is not marketed anywhere; it is supplied under investigational new drug exemptions, and adverse events reported so far have been mild and mostly unrelated to the drug (5 of 90 adverse events in the Essen trial were judged possibly related, none serious).","status":"phase-2","asOf":"2026-09-22","links":[{"label":"Pabst et al., Lancet Oncology 2025: 68Ga-FAPI-46 PET accuracy for cancer imaging with histopathology validation (phase 2 trial)","url":"https://pubmed.ncbi.nlm.nih.gov/40774265/"},{"label":"ClinicalTrials.gov NCT05160051 (68Ga-FAPI-46 PET for imaging of FAP-expressing cancer)","url":"https://clinicaltrials.gov/study/NCT05160051"},{"label":"ClinicalTrials.gov NCT05518903 (68Ga-FAPI-46 PET/CT for localised pancreatic ductal adenocarcinoma)","url":"https://clinicaltrials.gov/study/NCT05518903"}],"tags":["FAP","stroma","investigational"],"related":["ga-68"],"indications":["pancreatic-net","nsclc"],"sections":[],"technologies":["fapi-pet","pet-ct"],"targets":["fap"],"drugs":[],"companies":["ge-healthcare"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"A quinoline-based fibroblast activation protein (FAP) inhibitor labelled with gallium-68. It binds tightly and is largely internalised by FAP-expressing cancer-associated fibroblasts in the tumour stroma, which surround the actual cancer cells in most solid epithelial tumours; the label therefore highlights the stromal reaction to a tumour rather than the tumour cells themselves.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ga68-psma-11","kind":"drug","name":"Gallium-68 gozetotide (PSMA-11)","aka":[],"tldr":"Gallium-68 PSMA-11 was the first PSMA PET tracer approved in the US (2020), and is made on site from a generator or cyclotron.","summary":"Gallium-68 gozetotide (PSMA-11) is a 68Ga-labelled urea-based ligand that binds prostate-specific membrane antigen, lighting up prostate cancer on PET wherever it has spread. It is made on site from a germanium-68 generator or cyclotron and used for initial staging of higher-risk disease, for biochemical recurrence, and to confirm PSMA expression before 177Lu-PSMA-617 therapy. The UCLA/UCSF academic NDA (2020) established PSMA PET in the US, followed by Telix's Illuccix kit (2021) and Gozellix (2025, longer shelf-life) and Novartis' Locametz (2022, companion for Pluvicto). It competes with 18F agents (Pylarify, Posluma) that offer central distribution and a longer half-life. Whether findings on PSMA PET should change treatment in the absence of outcome trials remains debated. In plain terms, it was the first PSMA PET tracer approved in the US.","status":"approved","asOf":"2026-09-27","links":[{"label":"Drugs@FDA: ANDA 216410, gallium Ga 68 gozetotide (RadioMedix)","url":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=216410"},{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Gallium-68%20gozetotide"}],"tags":[],"related":["f-18","ga-68","ge-68","lu-177"],"indications":["prostate"],"sections":[],"technologies":["psma-pet"],"targets":["psma"],"drugs":[],"companies":["telix","novartis","radiomedix"],"institutions":["ucla-jonsson","ucsf"],"pathways":[],"terms":[],"trials":["nct07052214"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Illuccix / Gozellix / Locametz","modality":"PET imaging agent","mechanism":"68Ga-labelled urea-based PSMA ligand.","approvals":[{"region":"US","year":2020,"indication":"PSMA PET (UCLA/UCSF NDA); kits 2021-2022"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2026-06-08","type":"approval","region":"US","note":"Gallium Ga 68 gozetotide from RadioMedix approved under an abbreviated new drug application, ANDA 216410 (original approval)","source":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=216410"}]},{"id":"ga-68-pentixafor","kind":"drug","name":"Gallium-68 pentixafor","aka":["68Ga-Pentixafor","Gallium (68Ga) boclatixafortide"],"tldr":"An experimental PET tracer that looks for a specific docking protein (CXCR4) that some blood cancers and a minority of solid tumours carry in excess. It is a research tool, not an approved scan.","summary":"68Ga-Pentixafor has been used in over 1,300 patients across more than 75 publications, mostly at academic centres (Memorial Sloan Kettering, Technical University of Munich, and others) under investigator INDs, with no serious adverse events reported to date. Its clearest oncology signal is in multiple myeloma, indolent lymphomas and myeloproliferative neoplasms, where CXCR4 overexpression on malignant plasma cells or lymphocytes gives high image contrast; a first proof-of-principle study in myeloproliferative neoplasms found bone-marrow SUVmean of 6.45 versus 4.44 in healthy controls.\n\nIn solid tumours the picture is more mixed: a retrospective series of 142 patients across 23 histologies found discernible CXCR4 uptake above blood pool in only 68% of scans, indicating that receptor expression is present but inconsistent outside the haematological setting. Beyond oncology, the tracer is also being explored for primary aldosteronism lateralisation and unstable atherosclerotic plaque, reflecting CXCR4's broader role in inflammation. It has not been submitted for marketing approval anywhere and remains supplied through academic radiopharmacies under IND/IMPD exemptions.","status":"phase-2","asOf":"2026-09-22","links":[{"label":"Advances in PET imaging of the CXCR4 receptor, Seminars in Nuclear Medicine 2023","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC10792730/"},{"label":"CXCR4-directed PET/CT with 68Ga-pentixafor in solid tumours (142 patients), 2023","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC10957681/"}],"tags":["CXCR4","myeloma","investigational"],"related":["ga-68"],"indications":[],"sections":[],"technologies":["pet"],"targets":["cxcr4"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"A cyclic peptide analogue of the chemokine CXCL12, radiolabelled with gallium-68, that binds the chemokine receptor CXCR4. CXCR4 is upregulated on the surface of several haematological cancers (multiple myeloma, lymphomas, myeloproliferative neoplasms) and, less consistently, in solid tumours, so uptake marks tissue with high receptor density.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ho-166-microspheres","kind":"drug","name":"Holmium-166 microspheres","aka":["QuiremSpheres","166Ho-PLLA microspheres"],"tldr":"Tiny plastic beads carrying a radioactive, slightly magnetic metal are injected into the artery feeding a liver tumour. Because the metal shows up on both nuclear scans and MRI, doctors can check exactly where the beads went.","summary":"QuiremSpheres are holmium-166-labelled poly-L-lactic acid microspheres for radioembolisation (SIRT) of unresectable liver tumours, developed at University Medical Center Utrecht and commercialised by Quirem Medical (later acquired by Terumo). Holmium-166 has a physical half-life of 26.8 hours, so more than 90% of the radiation dose is delivered within the first four days after administration.\n\nThe product received CE marking as an active implantable medical device in April 2015, and a matching low-activity test dose (QuiremScout, identical size and shape) was CE-marked in 2018-2019 to predict lung shunting and biodistribution before therapy. Holmium-166 emits both beta particles (for therapy) and a gamma photon, and is paramagnetic, which allows quantitative SPECT and MRI-based dosimetry after treatment, alongside the more usual post-treatment imaging used for yttrium-90 products.\n\nQuiremSpheres has not obtained FDA approval and is used in Europe and other CE-mark-recognising markets; NICE (UK) technology appraisal TA985 reviewed its use in advanced HCC. It is one of three commercially available liver radioembolisation microsphere products, alongside the yttrium-90 resin (SIR-Spheres) and glass (TheraSphere) microspheres.","status":"approved","asOf":"2026-09-22","links":[{"label":"Holmium-166 radioembolisation: current status and future perspectives, PMC 2022","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC9626412/"},{"label":"NICE TA985: QuiremSpheres for advanced HCC","url":"https://www.nice.org.uk/guidance/ta985/chapter/2-Information-about-QuiremSpheres"},{"label":"Terumo: QuiremScout CE mark announcement, 2019","url":"https://www.terumo.com/newsrelease/detail/20190107/234"}],"tags":["radioembolisation","liver","beta emitter","CE mark"],"related":["y-90-resin-microspheres","y-90-glass-microspheres","y-90","ho-166"],"indications":["hcc"],"sections":[],"technologies":["radioembolisation-tare"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"QuiremSpheres","modality":"radioembolisation","mechanism":"Poly-L-lactic acid (PLLA) microspheres loaded with holmium-166 (a beta emitter that also emits an imageable gamma photon and is paramagnetic, so uptake can be checked on SPECT or MRI as well as CT), infused through a hepatic artery catheter to treat unresectable liver tumours.","approvals":[{"region":"EU","year":2015,"indication":"Treatment of unresectable liver tumours (radioembolisation)"}],"mechanismSteps":[],"dosing":{"route":"Intra-arterial infusion into the hepatic artery via catheter","schedule":"Single administration, typically with a QuiremScout test dose beforehand for dosimetry","source":"https://www.nice.org.uk/guidance/ta985/chapter/2-Information-about-QuiremSpheres"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"hrs-4357","kind":"drug","name":"HRS-4357","aka":[],"tldr":"HRS-4357 is an experimental investigational agent whose form is not stated in the registry from Jiangsu HengRui Medicine in phase 3 trials for prostate cancer, aimed at PSMA.","summary":"HRS-4357 is an investigational agent whose form is not stated in the registry developed by Jiangsu HengRui Medicine. Its target is PSMA (the sponsor names PSMA (inferred from trial population)). ClinicalTrials.gov describes the intervention as: HRS-4357 injection are administered each time, with dosing for 4 to 6 cycles. It is the investigational product in 1 recruiting or active industry-led phase 2 and phase 3 interventional cancer trial, including the phase 3 study NCT07311694 (A Phase III Study Comparing HRS-4357 With Novel Androgen Receptor Pathway Inhibitors in Patients With Progressive, PSMA-Positive Metastatic Castration-Resistant Prostate Cancer), in prostate cancer. The largest, NCT07311694, plans to enrol 370 participants with primary completion expected 2027-12. Status reflects the highest phase registered on ClinicalTrials.gov; no efficacy results are recorded here.","status":"phase-3","asOf":"2026-09-11","links":[{"label":"ClinicalTrials.gov: trials of HRS-4357","url":"https://clinicaltrials.gov/search?intr=HRS-4357"}],"tags":["pipeline","ctgov-ingest"],"related":[],"indications":["prostate"],"sections":[],"technologies":[],"targets":["psma"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["nct07311694"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2 + sponsor pipeline pages)","editedOn":"2026-09-11"},"modality":"not stated (registered as a drug or biological on ClinicalTrials.gov)","mechanism":"Investigational agent whose form is not stated in the registry directed at PSMA, as stated in the ClinicalTrials.gov intervention record; the detailed mechanism is not stated.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"ibritumomab-tiuxetan","kind":"drug","name":"Ibritumomab tiuxetan","aka":["Y-90 ibritumomab","Zevalin therapeutic regimen"],"tldr":"Zevalin is an antibody carrying a radioactive isotope that seeks out CD20 on lymphoma cells. It treats follicular lymphoma that has relapsed and is given as a one-off consolidation after chemotherapy.","summary":"Ibritumomab tiuxetan was the first radioimmunotherapy approved by the FDA, in February 2002, for relapsed or refractory low-grade, follicular or transformed B-cell non-Hodgkin lymphoma including rituximab-refractory disease (Study 106-06: response in a majority of 54 rituximab-refractory patients), and in 2009 for consolidation after first-line chemotherapy in follicular lymphoma with a response (FIT trial: prolonged progression-free survival). The EU authorised Zevalin in 2004. Despite efficacy and a single-day treatment, use collapsed because of logistics between nuclear medicine and haematology, prolonged cytopenias and competition from rituximab maintenance and later agents; tositumomab (Bexxar) was discontinued in 2014. Severe cytopenias and infusion reactions carry boxed warnings.","status":"approved","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Ibritumomab_tiuxetan","links":[{"label":"US label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=ibritumomab%20tiuxetan"},{"label":"NCI drug page","url":"https://www.cancer.gov/about-cancer/treatment/drugs/ibritumomabtiuxetan"},{"label":"EPAR","url":"https://www.ema.europa.eu/en/medicines/human/EPAR/zevalin"}],"tags":["nci-list"],"related":["rituximab","y-90"],"indications":["follicular-lymphoma"],"sections":[],"technologies":["radioimmunotherapy"],"targets":["cd20"],"drugs":[],"companies":["acrotech-biopharma"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Zevalin","modality":"Radioimmunotherapy (yttrium-90 labelled anti-CD20 antibody)","mechanism":"Murine anti-CD20 IgG1 (the parent of rituximab) chelated via tiuxetan to yttrium-90; beta emission delivers radiation to CD20-positive B cells and neighbouring tumour cells (crossfire), given after rituximab to clear circulating B cells.","approvals":[{"region":"US","year":2002,"indication":"Relapsed or refractory low-grade, follicular or transformed B-cell NHL including rituximab-refractory follicular lymphoma"},{"region":"US","year":2009,"indication":"Consolidation after first-line chemotherapy in previously untreated follicular NHL"},{"region":"EU","year":2004,"indication":"Rituximab-relapsed or refractory CD20-positive follicular lymphoma; first-line consolidation added 2008"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"illuccix","kind":"drug","name":"Illuccix (kit for Ga-68 gozetotide)","aka":[],"tldr":"Telix's ready-to-label kit that lets any nuclear medicine department make the gallium PSMA scan for prostate cancer.","summary":"Illuccix was approved by the FDA in December 2021 for PET imaging of PSMA-positive lesions in men with suspected metastasis who are candidates for definitive therapy and in men with suspected recurrence based on rising PSA, and in 2025 the label was extended to selecting patients for PSMA radioligand therapy. Gozellix, a second-generation kit with longer post-labelling shelf life, was approved in 2025. Illuccix is also registered in Australia and several other markets. The kit format made PSMA PET available to centres without access to the cyclotron-produced 18F tracers.","status":"approved","asOf":"2026-09-10","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Illuccix"}],"tags":["test"],"related":["ga68-psma-11","locametz","pylarify","f-18","ga-68"],"indications":["prostate"],"sections":[],"technologies":["psma-pet","pet-ct"],"targets":["psma"],"drugs":["pluvicto"],"companies":["telix"],"institutions":[],"pathways":[],"terms":["biochemical-recurrence","theranostics"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["What a result means: PSMA-avid spots on the scan indicate prostate cancer deposits and decide between local treatment, systemic therapy or radioligand therapy."],"brand":"Illuccix / Gozellix","modality":"PET imaging agent kit (PSMA, gallium-68)","mechanism":"Kit for on-site labelling of PSMA-11 (gozetotide) with gallium-68 from a generator or cyclotron; the tracer binds PSMA on prostate cancer cells for PET imaging.","approvals":[{"region":"US","year":2021,"indication":"PSMA PET imaging in prostate cancer (initial staging with suspected metastasis; suspected recurrence)"},{"region":"Australia","year":2021,"indication":"PSMA PET imaging in prostate cancer"},{"region":"US","year":2025,"indication":"Gozellix kit; selection of patients for PSMA-targeted radioligand therapy"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"in-111-pentetreotide","kind":"drug","name":"Indium-111 pentetreotide","aka":["111In-pentetreotide","OctreoScan"],"tldr":"The original nuclear medicine scan for finding neuroendocrine tumours, used before PET scans like Ga-68 DOTATATE became available. It is still FDA-approved but has largely been superseded because PET gives sharper pictures with less radiation.","summary":"OctreoScan (kit for the preparation of indium In-111 pentetreotide) was approved by FDA in 1994 (NDA 020314) and is still marketed, now by Curium, as a two-vial kit that the radiopharmacy combines before injection. It is indicated for scintigraphic localisation of primary and metastatic neuroendocrine tumours bearing somatostatin receptors, at a recommended dose of 111 MBq (3 mCi) for planar imaging or 222 MBq (6 mCi) for SPECT.\n\nOctreoScan was the standard-of-care functional imaging test for neuroendocrine tumours for roughly two decades, but head-to-head studies have consistently shown that the newer PET tracers (68Ga-DOTATATE, 68Ga-DOTATOC, 64Cu-DOTATATE) detect more lesions with better spatial resolution and lower radiation dose, and most guideline bodies (SNMMI, ENETS) now favour SSTR-PET where it is available. OctreoScan remains relevant where PET access is limited, and it has a long track record: the label carries specific precautions for insulinoma patients, who can develop severe hypoglycaemia with unlabelled octreotide co-administration, and the finished radiopharmaceutical must be used within six hours of preparation.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Octreoscan (kit for the preparation of Indium In 111 Pentetreotide Injection)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/020314Orig1s000Lbl.pdf"}],"tags":["SSTR2","SPECT","legacy agent"],"related":["cu-64-dotatate","ga-68-dotatoc","ga68-dotatate","ga-68","in-111","cu-64"],"indications":["neuroendocrine","pancreatic-net","small-intestinal-net"],"sections":[],"technologies":["spect","spect-ct"],"targets":["sstr2"],"drugs":[],"companies":["curium"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"OctreoScan","modality":"SPECT tracer","mechanism":"Pentetreotide is an octreotide derivative conjugated to the chelator DTPA; once labelled with indium-111 it binds somatostatin receptor subtype 2 on neuroendocrine tumour cells. Because indium-111 is a gamma emitter rather than a positron emitter, imaging is by SPECT (or SPECT/CT) rather than PET.","approvals":[{"region":"US","year":1994,"indication":"Scintigraphic localisation of primary and metastatic neuroendocrine tumours bearing somatostatin receptors"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection, after radiolabelling the kit","schedule":"111 MBq (3 mCi) for planar imaging; 222 MBq (6 mCi) for SPECT imaging; use within 6 hours of preparation","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/020314Orig1s000Lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"i-123-mibg","kind":"drug","name":"Iobenguane I-123","aka":["123I-MIBG","AdreView","Iobenguane I 123 Injection"],"tldr":"An injectable tracer that mimics a stress hormone and gets taken up by certain nerve-related tumours, such as pheochromocytoma and childhood neuroblastoma, so a scan afterwards can show where they are.","summary":"AdreView (Iobenguane I 123 Injection) was approved by FDA in 2008 for detection of primary or metastatic pheochromocytoma or neuroblastoma as an adjunct to other diagnostic tests, and gained a second, unrelated cardiac indication in 2013 (assessment of myocardial sympathetic innervation in heart failure via the heart-to-mediastinum ratio). The adult dose is 10 mCi (370 MBq) IV, and patients require thyroid-blocking medication beforehand to prevent free iodine-123 accumulating in the thyroid.\n\nThe most common adverse reactions in the pivotal trials -- dizziness, rash, pruritus, flushing, headache and injection-site haemorrhage -- occurred in under 1.3% of patients, and the product is contraindicated only in known hypersensitivity to iobenguane or iobenguane sulfate. It contains benzyl alcohol as a preservative, which carries a specific warning against use in premature or low-birth-weight infants (\"gasping syndrome\"). In oncology, 123I-MIBG scintigraphy remains part of SNMMI/EANM guideline workups for pheochromocytoma/paraganglioma and paediatric neuroblastoma, though 18F-FDOPA and 68Ga-DOTATATE PET have overtaken it in sensitivity for many indications, and 131I-MIBG is the therapeutic counterpart used once MIBG uptake is confirmed.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: AdreView (Iobenguane I 123 Injection)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022290s005lbl.pdf"},{"label":"FDA supplemental approval letter, NDA 22-290 (2013 cardiac indication)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2013/022290orig1s001ltr.pdf"}],"tags":["MIBG","SPECT","pheochromocytoma","neuroblastoma"],"related":["i131-mibg","iobenguane-i-131","f-18","ga-68","i-123","i-131"],"indications":["pheochromocytoma-paraganglioma","neuroblastoma","metastatic-ppgl"],"sections":[],"technologies":["spect","mibg-theranostics"],"targets":[],"drugs":[],"companies":["ge-healthcare"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"AdreView","modality":"SPECT tracer","mechanism":"Iobenguane (meta-iodobenzylguanidine, MIBG) is structurally related to noradrenaline and is taken up by the noradrenaline transporter into sympathetic neurons and neuroendocrine cells derived from the neural crest, including pheochromocytoma, paraganglioma and neuroblastoma cells. Labelling with the gamma emitter iodine-123 allows whole-body gamma-camera or SPECT imaging.","approvals":[{"region":"US","year":2008,"indication":"Detection of primary or metastatic pheochromocytoma or neuroblastoma as an adjunct to other diagnostic tests"},{"region":"US","year":2013,"indication":"Scintigraphic assessment of myocardial sympathetic innervation in NYHA class II/III heart failure with LVEF <=35% (non-oncology indication)"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection over 1-2 minutes","schedule":"10 mCi (370 MBq) for patients >=16 years or <16 years and >=70 kg; weight-scaled dose otherwise; thyroid blockade required beforehand","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022290s005lbl.pdf"},"toxicity":[{"event":"Dizziness, rash, pruritus, flushing, headache or injection-site haemorrhage (combined)","anyGradePct":1.3,"source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022290s005lbl.pdf"}],"access":[],"regulatoryEvents":[]},{"id":"i-123-mibg-cardiac","kind":"drug","name":"Iobenguane I-123 (cardiac use)","aka":["I-123 MIBG","123I-mIBG"],"tldr":"A radioactive tracer that mimics the body's own \"fight or flight\" nerve chemical and is taken up by the nerve endings in heart muscle. In people with heart failure, comparing how much of it the heart holds onto against the surrounding chest tissue gives a read on how damaged the heart's nerve supply is, which relates to future risk.","summary":"AdreView (iobenguane I-123 injection) is a noradrenaline-analogue SPECT agent originally approved by the FDA in 2008 for detecting primary or metastatic phaeochromocytoma or neuroblastoma; a 2013 supplemental approval added a distinct cardiac indication (outside this record's oncology scope but the reason it is filed here as a cardiac agent): scintigraphic assessment of sympathetic innervation of the myocardium by measurement of the heart-to-mediastinum (H/M) uptake ratio in patients with NYHA class II or III heart failure and left ventricular ejection fraction 35% or less.\n\nIn this population, AdreView is labelled to help identify patients with lower one- and two-year mortality risk, indicated by an H/M ratio of 1.6 or greater (expected range 1.0-2.4); the label explicitly states its utility has not been established for selecting a therapeutic intervention, for monitoring response to therapy, or for identifying patients at high risk of death. The recommended adult dose is 10 mCi (370 MBq) by slow intravenous injection, with thyroid blockade (potassium iodide or perchlorate) beforehand to protect the thyroid from free iodine-123, and planar chest imaging beginning about 4 hours after injection, with optional SPECT.\n\nThis is a different mechanism and a different clinical question from the perfusion tracers in this file: it does not assess coronary blood flow or ischaemia, but the integrity of the heart's autonomic nerve supply, used as a risk-stratification adjunct in systolic heart failure rather than a coronary artery disease diagnostic.","asOf":"2026-09-22","links":[{"label":"FDA label: AdreView (iobenguane I 123 injection), 2020 revision","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022290s005lbl.pdf"},{"label":"FDA approval letter: supplemental NDA 22-290/S-001 (cardiac heart failure indication, 2013)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2013/022290orig1s001ltr.pdf"}],"tags":["SPECT","sympathetic innervation","heart failure"],"related":["i131-mibg","iobenguane-i-131","mibg-theranostics","i-123"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"AdreView","modality":"SPECT tracer","mechanism":"Iobenguane (metaiodobenzylguanidine, MIBG) is a noradrenaline analogue taken up by cardiac sympathetic nerve terminals through the same norepinephrine transporter (uptake-1) used by noradrenaline itself, then stored in neurosecretory vesicles. In failing hearts, sympathetic nerve terminals are damaged or down-regulated, reducing MIBG uptake and washout characteristics; the heart-to-mediastinum (H/M) uptake ratio on a planar image taken about 4 hours after injection quantifies how much sympathetic innervation remains, independent of coronary anatomy.","approvals":[{"region":"US","year":2008,"indication":"Detection of primary or metastatic pheochromocytoma or neuroblastoma as an adjunct to other diagnostic tests"},{"region":"US","year":2013,"indication":"Scintigraphic assessment of sympathetic innervation of the myocardium via heart-to-mediastinum ratio in NYHA class II-III heart failure with LVEF ≤ 35%, to help identify patients with lower 1- and 2-year mortality risk"}],"mechanismSteps":[],"dosing":{"route":"Slow intravenous injection over 1-2 minutes, after thyroid blockade","schedule":"10 mCi (370 MBq) for patients 16 years or older (or under 16 and ≥ 70 kg); weight-scaled dose for younger/lighter paediatric patients; planar chest imaging at about 4 hours post-injection, SPECT optional","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022290s005lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"iobenguane-i-131","kind":"drug","name":"Iobenguane I-131 (therapeutic)","aka":["131I-MIBG","Ultratrace iobenguane"],"tldr":"Azedra was a radioactive drug that homed in on adrenal-type tumours (phaeochromocytoma and paraganglioma) that could not be removed and delivered radiation from inside. It was approved in 2018 and discontinued by its maker in 2024.","summary":"High-specific-activity iobenguane I-131 (Azedra) was approved by the FDA in July 2018 for adults and children aged 12 and over with iobenguane scan-positive, unresectable, locally advanced or metastatic phaeochromocytoma or paraganglioma requiring systemic therapy, on a single-arm phase 2 study in which a quarter of patients halved their antihypertensive medication for at least six months and most had tumour control. It was the first approved therapy for these tumours. Progenics (later Lantheus) discontinued manufacture in 2024, so patients rely on compounded low-specific-activity 131I-MIBG or lutetium-177 dotatate. Myelosuppression, secondary MDS and leukaemia, hypothyroidism and renal toxicity were the main risks; the diagnostic-dose iobenguane (AdreView) is an imaging agent covered separately.","status":"withdrawn","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Iobenguane","links":[{"label":"US label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=iobenguane"},{"label":"NCI drug page","url":"https://www.cancer.gov/about-cancer/treatment/drugs/iobenguanei131"}],"tags":["nci-list"],"related":["lutathera","lu-177","i-131"],"indications":["neuroendocrine"],"sections":[],"technologies":["mibg-theranostics","radioligand-therapy"],"targets":[],"drugs":[],"companies":["lantheus"],"institutions":[],"pathways":[],"terms":["radioiodine-term"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["Phaeochromocytoma and paraganglioma have no cancer record yet; linked to neuroendocrine tumours."],"brand":"Azedra","modality":"Radiopharmaceutical therapy (beta and gamma emitter)","mechanism":"Noradrenaline analogue taken up by the noradrenaline transporter into chromaffin and neuroendocrine tumour cells; iodine-131 beta emission delivers targeted radiation.","approvals":[{"region":"US","year":2018,"indication":"Iobenguane scan-positive unresectable, locally advanced or metastatic phaeochromocytoma or paraganglioma in patients 12 and older (discontinued 2024)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"i-125-seeds","kind":"drug","name":"Iodine-125 brachytherapy seeds","aka":["I-125 seeds","125I permanent seed implants"],"tldr":"Tiny metal seeds containing a mildly radioactive form of iodine are permanently placed inside a tumour, most often the prostate, where they slowly release radiation over several months and then become harmless.","summary":"Iodine-125 brachytherapy seeds are titanium-encapsulated radionuclide sources used mainly for permanent low-dose-rate (LDR) interstitial brachytherapy of localised prostate cancer, and also for other accessible tumours of the head and neck, lung, pancreas and elsewhere, either as primary treatment or for residual disease after surgery. In the US, seeds such as Theragenics' I-Seed, Implant Sciences' I-Plant and similar products are cleared through the FDA's 510(k) premarket notification pathway (product code KXK, 21 CFR 892.5730) as substantially equivalent to earlier cleared brachytherapy sources; brachytherapy as a procedure does not itself require separate FDA approval.\n\nIodine-125 has a 59.4-day physical half-life and a mean photon energy of about 28 keV. For prostate monotherapy, published series correlate a minimum dose covering 90% of the prostate volume (D90) of at least 140 Gy with improved biochemical control; when combined with external-beam radiotherapy the typical prescription is lower, around 108-110 Gy. Seeds are implanted transperineally under transrectal ultrasound (and sometimes fluoroscopic or CT) guidance, either as loose seeds or linked (so-called stranded seeds) at regular intervals, and remain permanently in place, gradually becoming inert as the isotope decays.\n\nIodine-125 competes with palladium-103 and caesium-131 as LDR prostate brachytherapy isotopes; comparative series have found no clear difference in outcomes between iodine-125 and palladium-103 at three years. Because this is a device/source category with many manufacturers rather than a single branded drug, the record here covers the isotope and its clinical use rather than one company's product.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA 510(k) clearance letter: I-Plant Model 3500 iodine-125 brachytherapy seeds","url":"https://www.accessdata.fda.gov/cdrh_docs/pdf2/k023242.pdf"},{"label":"Prostate brachytherapy review, Translational Andrology and Urology 2018","url":"https://cdn.amegroups.cn/journals/amepc/files/journals/3/articles/18019/public/18019-PB1-3327-R2.pdf"}],"tags":["brachytherapy","prostate cancer","gamma/X-ray emitter","permanent implant"],"related":[],"indications":["prostate","prostate-high-risk"],"sections":[],"technologies":["ldr-seed-brachytherapy"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"brachytherapy source","mechanism":"Titanium-encapsulated seeds containing iodine-125, a low-energy gamma/X-ray emitter with a 59.4-day physical half-life, are permanently implanted (typically transperineally into the prostate under ultrasound guidance) to deliver low-dose-rate radiation from within the tumour over several months.","approvals":[],"mechanismSteps":[],"dosing":{"route":"Permanent transperineal interstitial implantation (typically prostate), or interstitial/surface application at other sites","schedule":"Single permanent implant; monotherapy target D90 approximately 140-160 Gy, or approximately 108-110 Gy when combined with external-beam radiotherapy","source":"https://cdn.amegroups.cn/journals/amepc/files/journals/3/articles/18019/public/18019-PB1-3327-R2.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"i-131-tositumomab","kind":"drug","name":"Iodine-131 tositumomab","aka":["Bexxar","tositumomab and I-131 tositumomab"],"tldr":"A cancer-targeting antibody carrying a radioactive form of iodine was used, as a single course, to treat a type of blood cancer called non-Hodgkin lymphoma. The manufacturer stopped selling it in 2014 because too few patients were using it.","summary":"The Bexxar therapeutic regimen combined tositumomab, an anti-CD20 murine IgG2a monoclonal antibody, with the same antibody radiolabelled with iodine-131. It was approved by the FDA in 2003 (and in Canada in 2005) for CD20-positive relapsed or refractory low-grade, follicular or transformed non-Hodgkin lymphoma in patients who had progressed during or after rituximab therapy, including rituximab-refractory disease. It was given as a single course only, comprising an unlabelled predose followed by a dosimetric and then a therapeutic dose of 131I-tositumomab, with activity individualised to deliver a specified total-body radiation dose.\n\nBexxar competed with the similar CD20-targeted radioimmunotherapy ibritumomab tiuxetan (Zevalin, labelled with yttrium-90). Despite comparable efficacy, Bexxar's use declined steadily after a 2006 peak: by 2012 only about 75 US patients received it in a year. GlaxoSmithKline announced in August 2013 that it would discontinue manufacture and sale of the regimen, citing projected declining sales and the availability of alternative therapies; marketing was formally withdrawn on 20 February 2014.\n\nBexxar is a useful cautionary example in the graph: an approved, effective radiopharmaceutical regimen withdrawn for commercial rather than safety reasons, illustrating how logistics (dosimetry visits, hospital nuclear-medicine capacity, competition from simpler agents) can end a therapy's market life even when clinical data support it.","status":"withdrawn","asOf":"2026-09-22","links":[{"label":"GSK: announcement of discontinuation, 6 August 2013","url":"https://pipelinereview.com/gsk-to-discontinue-manufacture-and-sale-of-the-bexxar-therapeutic-regimen-tositumomab-and-iodine-i-131-tositumomab/"},{"label":"JAMA Internal Medicine: Withdrawal of drugs for commercial reasons - tositumomab, 2014","url":"https://static1.squarespace.com/static/55550f38e4b0884d8d80118e/t/5565d1aae4b0660ba5b932e2/1432736170326/2014+-+Nov+-+JAMA+IM+-+Withdrawal+of+Drugs+for+Commercial+Reasons+-+Tositumomab.pdf"},{"label":"The rise and fall of iodine-131 tositumomab: Bexxar's story","url":"https://openmedscience.com/the-rise-and-fall-of-iodine-131-tositumomab-bexxars-story/"}],"tags":["radioimmunotherapy","lymphoma","withdrawn","beta and gamma emitter"],"related":["ibritumomab-tiuxetan","rituximab","i-131","y-90"],"indications":["follicular-lymphoma"],"sections":[],"technologies":["radioimmunotherapy"],"targets":["cd20"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Bexxar","modality":"radioimmunotherapy","mechanism":"An unlabelled anti-CD20 murine monoclonal antibody (tositumomab) dosing step to saturate normal B-cell sinks, followed by the same antibody labelled with iodine-131, which delivers combined beta and gamma radiation directly to CD20-expressing lymphoma cells as well as an antibody-dependent immune effect.","approvals":[{"region":"US","year":2003,"indication":"CD20-positive relapsed or refractory, low-grade, follicular, or transformed non-Hodgkin lymphoma progressing during or after rituximab therapy"},{"region":"CA","year":2005,"indication":"Same indication as the US approval"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2013-08-06","type":"withdrawal","region":"US/CA","note":"GlaxoSmithKline announced it would discontinue manufacture and sale of the Bexxar regimen, citing declining use (about 75 US patients in 2012) and available alternative therapies.","source":"https://pipelinereview.com/gsk-to-discontinue-manufacture-and-sale-of-the-bexxar-therapeutic-regimen-tositumomab-and-iodine-i-131-tositumomab/"},{"date":"2014-02-20","type":"withdrawal","region":"US/CA","note":"Marketing of the Bexxar therapeutic regimen formally discontinued.","source":"https://openmedscience.com/the-rise-and-fall-of-iodine-131-tositumomab-bexxars-story/"}]},{"id":"i-123-ioflupane","kind":"drug","name":"Ioflupane I-123","aka":["DaTscan","DaTSCAN","123I-FP-CIT"],"tldr":"A brain scan that shows how many dopamine-releasing nerve endings remain in a part of the brain called the striatum, helping tell shaking from Parkinson's-type disease apart from other kinds of tremor and from Alzheimer's-type memory loss.","summary":"Ioflupane I-123 (DaTscan in the US, DaTSCAN in the EU; GE Healthcare) was approved by the FDA in January 2011 and by the EMA in 2000. It is a SPECT radiopharmaceutical indicated as an adjunct to other diagnostic evaluations for striatal dopamine transporter visualisation in adult patients with suspected Parkinsonian syndromes, to help differentiate essential tremor from tremor due to Parkinson's disease, multiple system atrophy or progressive supranuclear palsy (the scan cannot distinguish between these three), and in adult patients to help differentiate probable dementia with Lewy bodies from Alzheimer's disease (it also cannot separate dementia with Lewy bodies from Parkinson's disease dementia).\n\nThe recommended dose is 111-185 MBq (3-5 mCi) given as a slow intravenous injection over at least 15-20 seconds; a thyroid-blocking agent (potassium iodide solution, Lugol's solution or potassium perchlorate) must be given at least one hour beforehand to limit thyroid uptake of free iodine-123. SPECT imaging is performed 3 to 6 hours after injection. Effective dose is about 3.9-4.6 mSv from a 185 MBq administration, depending on the dosimetry source.\n\nInterpretation is by visual (and increasingly semi-quantitative, using striatal binding ratios against normative databases) assessment of striatal uptake shape and intensity: a normal, symmetric comma- or crescent-shaped pattern argues against a parkinsonian syndrome, while reduced, asymmetric or absent putamen uptake supports one. Unlike amyloid PET, DAT SPECT does not currently gate access to any approved disease-modifying therapy; its clinical role remains diagnostic clarification, particularly in early or atypical presentations where tremor aetiology or the AD-versus-Lewy-body-dementia distinction is unclear on clinical grounds alone.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: DaTscan (ioflupane I 123 injection)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022454s010lbl.pdf"},{"label":"EMA EPAR product information: DaTSCAN","url":"https://www.ema.europa.eu/en/documents/product-information/datscan-epar-product-information_en.pdf"},{"label":"EMA EPAR summary: DaTSCAN","url":"https://www.ema.europa.eu/en/medicines/human/EPAR/datscan"}],"tags":["SPECT","diagnostic","neurology","movement disorder"],"related":["parkinsonian-syndromes","alzheimers-disease","ge-healthcare","i-123"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"DaTscan","modality":"SPECT tracer","mechanism":"An iodine-123 labelled cocaine analogue (N-omega-fluoropropyl-2beta-carbomethoxy-3beta-(4-iodophenyl)nortropane) that binds presynaptic dopamine transporters on striatal nerve terminals, allowing SPECT visualisation of dopaminergic neuron density.","approvals":[{"region":"US","year":2011,"indication":"Striatal dopamine transporter SPECT imaging as an adjunct in adults with suspected Parkinsonian syndromes, to help differentiate essential tremor from tremor due to Parkinsonian syndromes"},{"region":"EU","year":2000,"indication":"Detecting loss of functional dopaminergic neuron terminals in the striatum in clinically uncertain Parkinsonian syndromes, and to help differentiate probable dementia with Lewy bodies from Alzheimer's disease"}],"mechanismSteps":[],"dosing":{"route":"Slow intravenous injection (>=15-20 seconds)","schedule":"111-185 MBq (3-5 mCi) single dose; thyroid blockade at least 1 hour before injection; SPECT imaging 3-6 hours after injection","monitoring":"Visual assessment of striatal uptake pattern, often supported by semi-quantitative striatal binding ratio software against normative reference data","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/022454s010lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"iomab-b","kind":"drug","name":"Iomab-B","aka":["Apamistamab-I131","131I-apamistamab"],"tldr":"Iomab-B is Actinium's radioactive antibody that clears the bone marrow before a transplant for older patients with active relapsed acute myeloid leukaemia; the phase 3 SIERRA trial met its primary endpoint but the FDA asked for another study.","summary":"Iomab-B delivers iodine-131 to CD45-positive cells, allowing patients with relapsed or refractory acute myeloid leukaemia who would not tolerate conventional myeloablative conditioning to proceed to allogeneic transplant. In the phase 3 SIERRA trial, Iomab-B followed by transplant produced durable complete remission at six months in a substantially higher share of patients than conventional care. Actinium reported in 2024 that the FDA requested an additional randomised trial before filing, and it is seeking partners; the trial is recorded here.","status":"phase-3","asOf":"2026-09-16","links":[{"label":"ClinicalTrials.gov: trials of Iomab-B","url":"https://clinicaltrials.gov/search?intr=Iomab-B"}],"tags":["pipeline","ctgov-ingest"],"related":["i-131"],"indications":[],"sections":[],"technologies":["radioimmunotherapy","radioligand-therapy"],"targets":[],"drugs":[],"companies":["actinium-pharmaceuticals"],"institutions":[],"pathways":[],"terms":[],"trials":["nct02665065"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2, curated)","editedOn":"2026-09-16"},"modality":"Radioimmunotherapy conditioning agent (anti-CD45 antibody labelled with iodine-131)","mechanism":"An antibody against CD45, found on all white blood cells, carries iodine-131 to the marrow and leukaemia cells and ablates them in place of high-dose chemotherapy before a stem cell transplant.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"jnj-87189401","kind":"drug","name":"JNJ-87189401","aka":[],"tldr":"JNJ-87189401 is an experimental costimulatory agent from Janssen Research & Development in phase 3 trials for prostate cancer, aimed at PSMA.","summary":"JNJ-87189401 is a costimulatory agent developed by Janssen Research & Development. Its target is PSMA (the sponsor names PSMA / CD28). The sponsor states: A PSMA-CD28 costimulatory agent intended to enhance T-cell activation via PSMA engagement plus CD28 costimulation. It is the investigational product in 1 recruiting or active industry-led phase 2 and phase 3 interventional cancer trial, including the phase 3 study NCT07164443 (A Study of Pasritamig With or Without JNJ-87189401 Versus Placebo for Late Line Metastatic Castration-resistant Prostate Cancer (mCRPC)), in prostate cancer. The largest, NCT07164443, plans to enrol 1203 participants with primary completion expected 2028-08-18. Status reflects the highest phase registered on ClinicalTrials.gov; no efficacy results are recorded here.","status":"phase-3","asOf":"2026-09-11","links":[{"label":"ClinicalTrials.gov: trials of JNJ-87189401","url":"https://clinicaltrials.gov/search?intr=JNJ-87189401"}],"tags":["pipeline","ctgov-ingest"],"related":[],"indications":["prostate"],"sections":[],"technologies":[],"targets":["psma"],"drugs":[],"companies":["johnson-johnson"],"institutions":[],"pathways":[],"terms":[],"trials":["mcrpc"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2 + sponsor pipeline pages)","editedOn":"2026-09-11"},"modality":"costimulatory bispecific antibody (PSMA x CD28, per the sponsor's pipeline page)","mechanism":"A PSMA-CD28 costimulatory agent intended to enhance T-cell activation via PSMA engagement plus CD28 costimulation.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"pb-212-psv359","kind":"drug","name":"Lead-212 PSV359","aka":["[212Pb]PSV359","PSV359","PSV377 (imaging analogue)"],"tldr":"A drug that homes to the scaffolding cells tumours build around themselves, carrying a radioactive metal that fires alpha particles over a very short range. A matching scan version shows first whether a patient's tumour has the target.","summary":"PSV359 is Perspective Therapeutics' lead-212 radioligand against fibroblast activation protein alpha, the marker of cancer-associated fibroblasts. FAP-alpha is attractive because it is present in the stroma of most epithelial cancers and nearly absent from normal adult tissue, and because high expression tracks with poor prognosis in non-small cell lung, colorectal, pancreatic, gastric, mesothelioma, head and neck, oesophageal and ovarian cancers.\n\nThe first-in-human phase 1/2 study, NCT06710756, opened in April 2025 with a planned 112 participants and uses the pair directly: [203Pb]PSV359 to image and [212Pb]PSV359 to treat. Its original tumour list was pancreatic, gastric and gastro-oesophageal junction, oesophageal, colorectal and ovarian cancer and head and neck squamous cell carcinoma. On 14 September 2026 Perspective announced a clinical collaboration and supply agreement with Merck under which the trial is amended to add cohorts combining [212Pb]PSV359 with pembrolizumab in FAP-alpha-positive non-small cell lung cancer and colorectal cancer. That amendment is what puts an alpha-emitting radioligand into NSCLC, a tumour that radiopharmaceuticals have otherwise reached only as a diagnostic.\n\nPerspective guides initial phase 1/2a data in late 2026. Nothing has been published on activity in lung cancer, and the pipeline table still lists the programme's target disease simply as solid tumours.","status":"phase-1","asOf":"2026-09-23","links":[{"label":"Perspective Therapeutics: clinical collaboration and supply agreement with Merck to evaluate [212Pb]PSV359 with Keytruda in FAP-alpha positive solid tumours, 14 September 2026","url":"https://www.perspectivetherapeutics.com/pr/perspective-therapeutics-announces-clinical-collaboration-and-supply-agreement-with-merck-to-evaluate-212pbpsv359-in-combination-with-keytruda-pembrolizumab-in-fap-a-positive-solid-tumors"},{"label":"ClinicalTrials.gov NCT06710756: lead-212 PSV359 therapy for patients with solid tumours","url":"https://clinicaltrials.gov/study/NCT06710756"},{"label":"Perspective Therapeutics pipeline","url":"https://www.perspectivetherapeutics.com/pipeline/"}],"tags":["FAP","lead-212","alpha","NSCLC"],"related":["perspective-therapeutics","fap","fapi-pet","pb-212","pb-212-vmt-alpha-net","targeted-alpha-therapy","nsclc","merck","pembrolizumab"],"indications":["nsclc"],"sections":[],"technologies":[],"targets":["fap"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["nct06710756"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"PSV359","modality":"Alpha-emitting radioligand (FAP-alpha targeted)","mechanism":"A small-molecule ligand for fibroblast activation protein alpha, the protease on the cancer-associated fibroblasts that build the stroma of most epithelial tumours, carrying lead-212 as the payload. Lead-212 decays through bismuth-212 to deliver an alpha particle, depositing its energy over a few cell diameters, so the dose lands on the stromal scaffold and the tumour cells packed against it rather than on distant marrow. The same targeting molecule labelled with lead-203 or gallium-68, designated PSV377, images FAP-alpha expression, so a patient can be selected on a scan before being treated.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"pb-212-vmt-alpha-net","kind":"drug","name":"Lead-212 VMT-alpha-NET","aka":["212Pb-VMT-alpha-NET","[212Pb]VMT-α-NET","203Pb-VMT-alpha-NET (imaging analogue)"],"tldr":"A drug that targets a marker on neuroendocrine tumour cells is being tested with two versions of a radioactive metal: one lets doctors see where the tumour is on a scan, and the other delivers a strong, short-range dose of radiation to kill the tumour cells.","summary":"VMT-alpha-NET is Perspective Therapeutics' targeted alpha-particle therapy (TAT) programme for somatostatin receptor subtype 2 (SSTR2)-expressing neuroendocrine tumours (NETs), pheochromocytoma/paraganglioma and meningioma. The same peptide is labelled with lead-203 for SPECT/CT imaging (used to plan a patient-specific kidney radiation-dose limit) and with the alpha-emitting isotope lead-212 for therapy.\n\nThe ongoing multicentre, open-label phase 1/2a trial (ClinicalTrials.gov NCT05636618) is a dose-escalation and dose-expansion study in up to about 300 adult, PRRT-naive patients with unresectable or metastatic SSTR2-positive NETs, bronchial NETs, pheochromocytoma/paraganglioma, or meningioma; dosing is by intravenous infusion roughly every 8 weeks. The FDA granted Fast Track designation in September 2022 for SSTR2-positive NETs regardless of prior treatment. A separate single-centre phase 1 study in PRRT-refractory patients (NCT06148636) is under way at the University of Iowa.\n\nInterim data presented at ASCO-GI and AACR in 2026 (data cut-offs through April 2026) reported, across dose cohorts up to 64 patients, no dose-limiting toxicities, treatment-related discontinuations or grade 5 events, with grade 3+ adverse events in roughly a third of patients (mostly non-renal, non-myelosuppressive); in evaluable patients from the lower dose cohorts, 76% remained progression-free and alive, and an objective response rate of about 39-44% (RECIST v1.1) was reported in Cohort 2 (5 mCi per dose). VMT-alpha-NET has not received marketing authorisation in any jurisdiction; the programme is still determining its recommended phase 2 dose.","status":"phase-2","asOf":"2026-09-22","links":[{"label":"Perspective Therapeutics: VMT-alpha-NET pipeline page","url":"https://perspectivetherapeutics.com/pipeline/vmt-alpha-net"},{"label":"ClinicalTrials.gov: NCT05636618","url":"https://clinicaltrials.gov/study/NCT05636618"},{"label":"Perspective Therapeutics: updated interim data at AACR 2026","url":"https://www.globenewswire.com/news-release/2026/04/20/3276793/0/en/perspective-therapeutics-presents-updated-interim-data-of-212pb-vmt-%CE%B1-net-in-its-ongoing-phase-1-2a-clinical-trial-at-the-2026-aacr-annual-meeting.html"},{"label":"Perspective Therapeutics: first patient dosed press release, 2023","url":"https://perspectivetherapeutics.com/pr/perspective-therapeutics-announces-first-patient-dosed-in-a-phase-1-study-of-212pbvmtnet-to-treat-refractory-or-relapsedneuroendocrine-tumors"}],"tags":["alpha therapy","SSTR2","neuroendocrine tumours","lead-212","phase 1/2"],"related":["alphamedix","itm-11","lutathera","pb-212"],"indications":["neuroendocrine"],"sections":[],"technologies":["targeted-alpha-therapy"],"targets":["sstr2"],"drugs":[],"companies":["perspective-therapeutics"],"institutions":[],"pathways":[],"terms":[],"trials":["nct05636618"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"VMT-alpha-NET","modality":"alpha therapy","mechanism":"A somatostatin receptor subtype 2 (SSTR2)-targeting peptide that can be radiolabelled either with lead-203 (a gamma emitter, for SPECT imaging and dosimetry planning) or with lead-212 (an in-vivo alpha-emitter generator via its decay chain), delivering high-linear-energy-transfer alpha radiation directly to SSTR2-expressing neuroendocrine tumour cells.","approvals":[],"mechanismSteps":[],"dosing":{"route":"Intravenous infusion","schedule":"Dose-escalation cohorts from 2.5 to 6.0 mCi per dose, approximately every 8 weeks, up to 4 administrations","source":"https://www.globenewswire.com/news-release/2026/04/20/3276793/0/en/perspective-therapeutics-presents-updated-interim-data-of-212pb-vmt-%CE%B1-net-in-its-ongoing-phase-1-2a-clinical-trial-at-the-2026-aacr-annual-meeting.html"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"locametz","kind":"drug","name":"Locametz (kit for Ga-68 gozetotide)","aka":[],"tldr":"Novartis' gallium PSMA scan kit, approved the same day as Pluvicto as the test that qualifies men for that radioactive drug.","summary":"Locametz was approved by the FDA on 23 March 2022, alongside Pluvicto (lutetium-177 vipivotide tetraxetan), with an explicit indication for selecting patients with metastatic castration-resistant prostate cancer for PSMA-directed therapy, as well as for initial staging and biochemical recurrence. The European Commission approved it in December 2022. It is manufactured by Advanced Accelerator Applications, the Novartis radiopharmaceutical unit, and was the first PSMA PET agent approved in the EU. The scan-then-treat pairing is the template for theranostics.","status":"approved","asOf":"2026-09-10","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Locametz"}],"tags":["test"],"related":["ga68-psma-11","illuccix","ga-68","lu-177"],"indications":["prostate"],"sections":[],"technologies":["psma-pet","pet-ct","radioligand-therapy"],"targets":["psma"],"drugs":["pluvicto"],"companies":["novartis","advanced-accelerator-applications"],"institutions":[],"pathways":[],"terms":["theranostics"],"trials":["vision"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["What a result means: enough PSMA uptake on the scan is required before Pluvicto can be given; a scan without uptake means the drug is unlikely to work."],"brand":"Locametz","modality":"PET imaging agent kit (PSMA, gallium-68)","mechanism":"Kit for on-site labelling of gozetotide (PSMA-11) with gallium-68; the resulting tracer images PSMA-expressing prostate cancer and identifies candidates for lutetium-177 PSMA therapy.","approvals":[{"region":"US","year":2022,"indication":"PSMA PET in prostate cancer, including selection of patients for PSMA radioligand therapy"},{"region":"EU","year":2022,"indication":"PSMA PET in prostate cancer"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"lutathera","kind":"drug","name":"Lutetium-177 dotatate","aka":[],"tldr":"Lutetium-177 dotatate was the first modern radioligand therapy (2018), for neuroendocrine tumours, and is now used in first line.","summary":"Lutetium-177 dotatate is a radioligand therapy: the somatostatin analogue DOTATATE binds SSTR2 on neuroendocrine tumour cells and carries the beta emitter 177Lu into them, irradiating over a few millimetres. NETTER-1 established it in midgut NETs progressing on octreotide, and NETTER-2 (2024) moved it into first line for higher grade-2 and grade-3 GEP-NETs with PFS 22.8 versus 8.5 months. It was approved in 2018 for SSTR-positive GEP-NETs, with paediatric use from age 12 added in 2024. Dosing is 7.4 GBq every 8 weeks for 4 doses with an amino acid infusion to protect the kidneys; lymphopenia is common, and myelodysplastic syndrome (2.3%) and acute leukaemia (0.5%) are rare late risks. Alpha-emitting successors RYZ101 and AlphaMedix are in phase 3. The first generic is queued behind the patents: on 21 September 2026 FDA tentatively approved Lantheus's ANDA 217060 (Bravnetsa, 10 mCi/mL), finding it bioequivalent to Lutathera (NDA 208700), but withheld final approval because Advanced Accelerator Applications (Novartis) is suing Lantheus over US patent 10,596,276 in the District of Delaware (Civil Action No. 24-00095); final approval waits for the 30-month stay to run out, a court ruling that the patent is invalid or not infringed, or the patent's expiry on 25 January 2039. For a newcomer: the first modern radioligand therapy and the template for a whole class.","status":"approved","asOf":"2026-10-04","wikipedia":"https://en.wikipedia.org/wiki/Lutetium_(177Lu)_oxodotreotide","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Lutetium-177%20dotatate"},{"label":"Drugs@FDA: ANDA 217060, Bravnetsa (Lantheus), tentative approval","url":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=217060"},{"label":"FDA tentative approval letter, ANDA 217060 (21 Sep 2026)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2026/217060Orig1s000TAltr.pdf"}],"tags":[],"related":["lu-177"],"indications":["neuroendocrine","small-intestinal-net","pancreatic-net","grade-3-net","metastatic-ppgl"],"sections":[],"technologies":["radioligand-therapy"],"targets":["sstr2"],"drugs":[],"companies":["novartis"],"institutions":[],"pathways":[],"terms":["prrt-term"],"trials":["netter-1","nct04711135","nct05142696","nct03972488"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Lutathera","code":"177Lu-DOTATATE","modality":"Radioligand therapy (beta)","mechanism":"SSTR2 agonist peptide with 177Lu.","approvals":[{"region":"US","year":2018,"indication":"SSTR+ GEP-NETs"},{"region":"US","year":2024,"indication":"Paediatric ≥12 years; first-line (NETTER-2 label)"},{"region":"EU","year":2017,"indication":"First approval globally (Sep 2017)"}],"mechanismSteps":["Radioligand circulates and binds Somatostatin receptor 2 on tumour cells","Ligand is internalised or retained at the membrane","Beta emissions deposit energy within a short range","Clustered DNA double-strand breaks form in the tumour cell and its neighbours (crossfire)","Cells die; unbound ligand is cleared via the kidneys"],"dosing":{"route":"IV infusion","schedule":"7.4 GBq (200 mCi) every 8 weeks for 4 doses, with amino acid infusion starting 30 minutes before and continuing ≥3 hours","modifications":"Hold for grade ≥3 haematologic toxicity or renal toxicity; discontinue after 16-week delay","monitoring":"Blood counts, creatinine, LFTs before each dose; long-term MDS/AML surveillance","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55"},"toxicity":[{"event":"Lymphopenia","grade3PlusPct":44,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"GGT increased","grade3PlusPct":20,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"Vomiting","grade3PlusPct":7,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"Nausea","grade3PlusPct":5,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"AST increased","grade3PlusPct":5,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"ALT increased","grade3PlusPct":4,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"Hyperglycaemia","grade3PlusPct":4,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"Hypokalaemia","grade3PlusPct":4,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"},{"event":"Myelodysplastic syndrome","anyGradePct":2.3,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"Median onset 29 months"},{"event":"Acute leukaemia","anyGradePct":0.5,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=72d1a024-00b7-418a-b36e-b2cb48f2ab55","note":"NETTER-1; grade 3-4 rates"}],"access":[{"country":"US","listPrice":"~$47,500 per dose (launch price 2018)","reimbursement":"Medicare Part B (physician-administered); commercial plans per formulary","source":"https://www.cms.gov/medicare/payment/part-b-drugs/asp-pricing-files","asOf":"2026-09-06"},{"country":"UK","reimbursement":"NICE: recommended for unresectable/metastatic GEP-NETs (TA539)","source":"https://www.nice.org.uk/guidance/published?ngt=Technology%20appraisal%20guidance","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2017-09-26","type":"approval","region":"EU","note":"EMA approval: first modern PRRT","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2018-01-26","type":"approval","region":"US","note":"SSTR+ gastroenteropancreatic NETs (NETTER-1)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2024-04-23","type":"approval","region":"US","note":"Paediatric patients ≥12 years","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2024-06","type":"label-change","region":"US","note":"First-line label based on NETTER-2","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},{"id":"lu-177-dotatate-generic","kind":"drug","name":"Lutetium-177 dotatate (radioligand equivalent)","aka":["Bexlutry","generic lutetium Lu 177 dotatate"],"tldr":"A second, cheaper version of an already-approved radioactive drug for neuroendocrine tumours has been approved, using the same active radioactive ingredient as the original but made by a different company.","summary":"Bexlutry (lutetium Lu 177 dotatate injection), from Curium, is the first product the FDA has approved as a 'radioligand equivalent' of an existing radiopharmaceutical: it has the same active radiopharmaceutical ingredient as Novartis/Advanced Accelerator Applications' Lutathera. The FDA approved it on 14 September 2026 for adults with somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumours (GEP-NETs), spanning foregut, midgut and hindgut tumours.\n\nCurium filed under the FDA's 505(b)(2) pathway in July 2024, relying on published evidence and bridging data demonstrating a similar biological and chemical profile to Lutathera rather than running a new phase 3 trial. Approval followed a June 2026 court decision that cleared Curium of patent-infringement claims brought by Novartis. Unlike Lutathera, whose US label also covers paediatric patients aged 12 and older, Bexlutry's approval is adult-only.\n\nBexlutry is immediately available for prescribing in the US. A second lutetium dotatate candidate, Lantheus's PNT2003, received FDA tentative approval in March 2026 under the abbreviated new drug application (ANDA) pathway but is not yet launched; separately, ITM's related product 177Lu-edotreotide (ITM-11) received an FDA complete response letter in August 2026 over manufacturing and third-party facility issues unrelated to its clinical data. Bexlutry's approval is the first time a radioligand therapy for cancer has faced this kind of direct, lower-cost competition in the US market.","status":"approved","asOf":"2026-09-27","links":[{"label":"Drugs@FDA: NDA 218525, Bexlutry (lutetium Lu 177 dotatate)","url":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=218525"},{"label":"Curium: FDA approval of BEXLUTRY, 14 September 2026","url":"https://www.curiumpharma.com/2026/09/14/fda-approval-bexlutry/"},{"label":"FiercePharma: FDA approves first radioligand equivalent","url":"https://www.fiercepharma.com/pharma/fda-approves-first-radioligand-equivalent-curiums-copycat-novartis-lutathera"},{"label":"MedPath: FDA approves Curium's Bexlutry, first generic radioligand","url":"https://trial.medpath.com/news/fda-approves-curium-s-bexlutry-first-generic-radioligand-challenging-lutathera-s-gep-net-monopoly"}],"tags":["radioligand therapy","generic","neuroendocrine tumours","beta emitter"],"related":["lutathera","itm-11","lu-177"],"indications":["neuroendocrine","pancreatic-net","small-intestinal-net"],"sections":[],"technologies":["radioligand-therapy","prrt"],"targets":["sstr2"],"drugs":[],"companies":["curium"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Bexlutry","modality":"radioligand therapy","mechanism":"A somatostatin analogue (DOTATATE) labelled with beta-emitting lutetium-177, delivering targeted radiation to somatostatin receptor-positive neuroendocrine tumour cells; chemically and biologically the same active ingredient as Lutathera, approved through the FDA's 505(b)(2) route as a radioligand equivalent rather than through a new pivotal efficacy trial.","approvals":[{"region":"US","year":2026,"indication":"Somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumours (GEP-NETs), including foregut, midgut and hindgut tumours, in adults","note":"Approved via the FDA 505(b)(2) pathway as a radioligand equivalent of Lutathera, 14 September 2026"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2026-09-14","type":"approval","region":"US","note":"Bexlutry, NDA 218525 (Curium), original approval; FDA classification Type 5 new formulation or new manufacturer, standard review","source":"https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=218525"}]},{"id":"lu-177-pnt2002","kind":"drug","name":"Lutetium-177 PNT2002","aka":["177Lu-PNT2002","177Lu-PSMA-I&T (POINT/Lantheus)"],"tldr":"A radioactive drug that homes in on a marker found on most prostate cancer cells, delivering radiation directly to the tumour, is being tested as a treatment for prostate cancer that has stopped responding to hormone therapy.","summary":"177Lu-PNT2002 is a PSMA-targeted radioligand therapy built on the PSMA-I&T ligand, labelled with beta-emitting no-carrier-added lutetium-177. POINT Biopharma developed it and Lantheus in-licensed exclusive worldwide commercial rights (excluding certain Asian territories) in December 2022; POINT was subsequently acquired by Eli Lilly. The FDA granted Fast Track designation for metastatic castration-resistant prostate cancer (mCRPC) in April 2023.\n\nThe pivotal phase 3 SPLASH trial (NCT04647526) randomised 412 patients with PSMA-expressing mCRPC who had progressed on an androgen receptor pathway inhibitor (ARPI) and refused or were ineligible for chemotherapy, 2:1 to 177Lu-PNT2002 (up to four cycles, 6.8 GBq per cycle every 8 weeks) versus a change to abiraterone or enzalutamide, with crossover allowed on progression. Topline results (December 2023) showed a statistically significant improvement in radiographic progression-free survival by blinded independent central review: median 9.5 months with 177Lu-PNT2002 versus 6.0 months with ARPI (HR 0.71, p=0.0088); overall survival was immature, with an interim HR of 1.11, and 84.6% of control-arm patients who progressed crossed over. Grade 3+ treatment-emergent adverse events, serious adverse events and discontinuations for toxicity were all numerically lower on 177Lu-PNT2002 than on ARPI.\n\nAs of the March 2026 status, 177Lu-PNT2002 has not received a marketing authorisation in any jurisdiction; further follow-up data were expected in 2024 ahead of a potential US new drug application.","status":"phase-3","asOf":"2026-09-22","links":[{"label":"Lantheus/POINT: positive topline SPLASH results, 18 December 2023","url":"https://lantheusholdings.gcs-web.com/news-releases/news-release-details/lantheus-and-point-biopharma-announce-positive-topline-results"},{"label":"FDA Fast Track designation announcement, 24 April 2023","url":"https://investor.lantheus.com/node/14596/pdf"},{"label":"Initial clinical experience with 177Lu-PNT2002 (SPLASH lead-in), PMC 2025","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC11745944/"},{"label":"ClinicalTrials.gov: SPLASH (NCT04647526)","url":"https://clinicaltrials.gov/study/NCT04647526"}],"tags":["PSMA","radioligand therapy","prostate cancer","beta emitter","phase 3"],"related":["pluvicto","lu177-psma-it","lu-177"],"indications":["prostate-mcrpc"],"sections":[],"technologies":["radioligand-therapy"],"targets":["psma"],"drugs":[],"companies":["lantheus","point-biopharma","eli-lilly"],"institutions":[],"pathways":[],"terms":[],"trials":["splash"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"PNT2002","modality":"radioligand therapy","mechanism":"A PSMA-targeted small-molecule ligand (PSMA-I&T) labelled with no-carrier-added lutetium-177, a beta emitter, delivering targeted radiation to PSMA-expressing prostate cancer cells after intravenous infusion.","approvals":[],"mechanismSteps":[],"dosing":{"route":"Intravenous infusion","schedule":"Up to 4 cycles at 6.8 GBq (±10%) per cycle, every 8 weeks (SPLASH trial regimen)","source":"https://pmc.ncbi.nlm.nih.gov/articles/PMC11745944/"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tlx-591","kind":"drug","name":"Lutetium-177 rosopatamab tetraxetan","aka":["TLX591","TLX591-Tx","177Lu-rosopatamab tetraxetan"],"tldr":"A cancer-targeting antibody carrying a radioactive metal is being tested as a two-dose treatment for advanced prostate cancer, on top of the usual hormone or chemotherapy drugs.","summary":"TLX591 (INN lutetium Lu 177 rosopatamab tetraxetan; also referred to as TLX591-Tx) is Telix Pharmaceuticals' lead PSMA-targeted radio-antibody-drug conjugate for metastatic castration-resistant prostate cancer (mCRPC). Unlike small-molecule PSMA ligands (e.g. PSMA-617, PSMA-I&T), TLX591 uses a full-length PSMA-targeting monoclonal antibody, given as two 76 mCi intravenous infusions 14 days apart; its hepatic (rather than renal) clearance means long-term follow-up has not shown significant acute or delayed nephrotoxicity.\n\nBy the ProstACT SELECT trial (NCT04786847), 242 patients had been treated with TLX591 across eight phase 1/2 studies; SELECT itself reported a median radiographic progression-free survival of 8.8 months in 23 evaluable mCRPC patients, and an earlier single-arm phase 2 study reported 42.3-month overall survival in 17 patients dosed under a fractionated regimen with concurrent docetaxel.\n\nThe pivotal phase 3 ProstACT Global trial (ClinicalTrials.gov NCT06520345) compares TLX591-Tx plus standard of care (abiraterone, enzalutamide or docetaxel) against standard of care alone in PSMA-positive mCRPC patients who progressed on one prior ARPI, with an initial 36-patient safety/dosimetry lead-in (Part 1) followed by a 2:1 randomised expansion (Part 2, target enrolment approximately 490). Part 1 results (reported March 2026) showed an acceptable safety and tolerability profile across all three standard-of-care combination cohorts, with no new safety signals; the main non-haematological toxicities were fatigue, nausea and dry mouth, and haematological toxicity (thrombocytopenia, neutropenia) was transient and manageable. Part 2 is enrolling in Australia, New Zealand, Canada, Türkiye, the UK and other jurisdictions; TLX591 has not yet received marketing authorisation anywhere.","status":"phase-3","asOf":"2026-09-22","links":[{"label":"Telix: first patient dosed in ProstACT GLOBAL Phase 3","url":"https://telixpharma.com/news-views/first-patient-dosed-in-phase-iii-prostact-global-study-of-antibody-based-prostate-cancer-therapy-candidate-tlx591/"},{"label":"Telix: ProstACT Global Part 1 achieves primary objectives, 9 March 2026","url":"https://telixpharma.com/news-views/prostact-global-phase-3-study-part-1-achieves-primary-objectives/"},{"label":"Telix: positive rPFS data from ProstACT SELECT trial","url":"https://telixpharma.com/wp-content/uploads/2024/05/TLX_ProstACT_SELECT_Study_of_TLX591_rADC_Therapy_Positive_rPFS.pdf"},{"label":"ClinicalTrials.gov: ProstACT Global (NCT06520345)","url":"https://clinicaltrials.gov/study/NCT06520345"}],"tags":["PSMA","radio-antibody-drug conjugate","prostate cancer","phase 3"],"related":["illuccix","pluvicto","lu-177"],"indications":["prostate-mcrpc"],"sections":[],"technologies":["radioimmunotherapy"],"targets":["psma"],"drugs":[],"companies":["telix"],"institutions":[],"pathways":[],"terms":[],"trials":["nct06520345"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"code":"TLX591","modality":"radioimmunotherapy","mechanism":"A radio-antibody-drug conjugate (rADC): a high-specificity PSMA-targeting monoclonal antibody, linked via a chelator to cytotoxic lutetium-177, given intravenously. Because it is a full antibody rather than a small molecule, it has longer tumour retention and different biodistribution to small-molecule PSMA radioligands, with lower observed uptake in kidneys, salivary and lacrimal glands.","approvals":[],"mechanismSteps":[],"dosing":{"route":"Intravenous infusion","schedule":"Two doses of 76 mCi, 14 days apart, per treatment course","source":"https://telixpharma.com/wp-content/uploads/2024/05/TLX_ProstACT_SELECT_Study_of_TLX591_rADC_Therapy_Positive_rPFS.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"pluvicto","kind":"drug","name":"Lutetium-177 vipivotide tetraxetan","aka":[],"tldr":"A radioactive drug that seeks out PSMA on prostate cancer cells; the best-selling radiopharmaceutical ever.","summary":"VISION (2021): OS 15.3 vs 11.3 months in post-chemotherapy mCRPC. PSMAfore (2023) led to a 2025 label before chemotherapy. July 2026 FDA action further expanded the label (per AACR/FDA roundups). PSMAddition tests it in hormone-sensitive disease. Requires PSMA PET positivity. Six cycles every 6 weeks; xerostomia, cytopenias, renal monitoring.","status":"approved","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Lutetium_(177Lu)_vipivotide_tetraxetan","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Lutetium-177%20vipivotide%20tetraxetan"}],"tags":[],"related":["lu-177"],"indications":["prostate","prostate-mcrpc","prostate-mhspc"],"sections":[],"technologies":["radioligand-therapy","psma-pet"],"targets":["psma"],"drugs":[],"companies":["novartis"],"institutions":[],"pathways":[],"terms":[],"trials":["vision","psmafore","nct05682443","nct06894511","nct06004661"],"people":["louise-emmett"],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Pluvicto","code":"177Lu-PSMA-617","modality":"Radioligand therapy (beta)","mechanism":"Small-molecule PSMA ligand chelated to 177Lu; beta emission with 2 mm range.","approvals":[{"region":"US","year":2022,"indication":"PSMA+ mCRPC after ARPI and taxane"},{"region":"US","year":2025,"indication":"PSMA+ mCRPC after ARPI, before chemotherapy"},{"region":"US","year":2026,"indication":"Label expansion (July 2026)"},{"region":"EU","year":2022,"indication":"mCRPC post-ARPI and taxane; pre-chemo 2025"}],"mechanismSteps":["Radioligand circulates and binds PSMA on tumour cells","Ligand is internalised or retained at the membrane","Beta emissions deposit energy within a short range","Clustered DNA double-strand breaks form in the tumour cell and its neighbours (crossfire)","Cells die; unbound ligand is cleared via the kidneys"],"dosing":{"route":"IV injection","schedule":"7.4 GBq (200 mCi) every 6 weeks for up to 6 doses","modifications":"Hold for grade ≥3 myelosuppression or renal impairment; permanently discontinue for grade 4 haematologic toxicity","monitoring":"Blood counts and renal function before each dose; hydration; radiation-protection instructions for 7 days","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a"},"toxicity":[{"event":"Lymphocytes decreased","anyGradePct":85,"grade3PlusPct":47,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a","note":"VISION"},{"event":"Haemoglobin decreased","anyGradePct":64,"grade3PlusPct":15,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a","note":"VISION"},{"event":"Fatigue","anyGradePct":48,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a","note":"VISION"},{"event":"Dry mouth","anyGradePct":39,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a","note":"VISION"},{"event":"Nausea","anyGradePct":36,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a","note":"VISION"},{"event":"Decreased appetite","anyGradePct":21,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a","note":"VISION"},{"event":"Platelets decreased","grade3PlusPct":9,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=14908037-2892-4d98-a053-253ce35afb1a","note":"VISION"}],"access":[{"country":"US","listPrice":"~$42,500 per dose (Novartis, 2022 launch price)","reimbursement":"Medicare Part B (physician-administered); commercial plans per formulary","assistance":"https://www.novartis.com/us-en/patient-support","source":"https://www.cms.gov/medicare/payment/part-b-drugs/asp-pricing-files","asOf":"2026-09-06"},{"country":"UK","reimbursement":"NICE: recommended for PSMA+ mCRPC after ARPI and taxane (2025); pre-chemotherapy appraisal in progress","source":"https://www.nice.org.uk/guidance/published?ngt=Technology%20appraisal%20guidance","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2021-06","type":"designation","region":"US","note":"Breakthrough Therapy designation","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2022-03-23","type":"approval","region":"US","note":"PSMA+ mCRPC after ARPI and taxane (VISION)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2022-12","type":"approval","region":"EU","note":"EMA approval","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2025-03-28","type":"approval","region":"US","note":"PSMA+ mCRPC after ARPI, before chemotherapy (PSMAfore)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2026-07-31","type":"approval","region":"US","note":"PSMA+ metastatic hormone-sensitive prostate cancer with ARPI (PSMAddition)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},{"id":"olaparib","kind":"drug","name":"Olaparib","aka":[],"tldr":"Olaparib was the first PARP inhibitor, and turned an inherited BRCA mutation from a risk factor into a drug target, including after surgery in breast cancer.","summary":"Approved 2014 (ovarian), then maintenance first-line (SOLO-1, 7-year OS benefit), with bevacizumab (PAOLA-1, HRD+), metastatic BRCA breast (OlympiAD), adjuvant germline-BRCA HER2-negative early breast cancer (OlympiA, OS HR 0.72), pancreatic maintenance (POLO), and prostate (PROfound; PROpel with abiraterone). AstraZeneca/Merck.","status":"approved","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Olaparib","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Olaparib"}],"tags":[],"related":[],"indications":["prostate","prostate-mcrpc"],"sections":[],"technologies":[],"targets":["parp"],"drugs":[],"companies":["astrazeneca","merck"],"institutions":[],"pathways":[],"terms":[],"trials":["nct06909825"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Lynparza","modality":"Small-molecule PARP inhibitor","mechanism":"PARP1/2 inhibitor and trapper; synthetic lethality with HRD.","approvals":[{"region":"US","year":2014,"indication":"gBRCA ovarian cancer ≥3 lines"},{"region":"US","year":2018,"indication":"gBRCA HER2- metastatic breast cancer"},{"region":"US","year":2022,"indication":"Adjuvant gBRCA high-risk HER2- early breast cancer"}],"mechanismSteps":["Olaparib binds PARP1/2 at sites of single-strand DNA breaks","PARP is trapped on DNA and repair of single-strand breaks stops","Replication forks collide with trapped PARP and collapse into double-strand breaks","BRCA-deficient cells cannot repair the breaks by homologous recombination","Genomic catastrophe and apoptosis in tumour cells; normal cells with intact BRCA survive"],"dosing":{"route":"Oral","schedule":"300 mg twice daily; 1 year adjuvant (OlympiA); 2 years first-line ovarian maintenance; until progression otherwise","modifications":"200 mg BID for moderate renal impairment; hold for grade ≥3 anaemia; discontinue for MDS/AML or pneumonitis","monitoring":"Blood counts monthly; respiratory symptoms; embryo-fetal counselling","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa"},"toxicity":[{"event":"Nausea","anyGradePct":57,"grade3PlusPct":0.8,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"Fatigue","anyGradePct":42,"grade3PlusPct":1.8,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"Anaemia","anyGradePct":24,"grade3PlusPct":9,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"Vomiting","anyGradePct":23,"grade3PlusPct":0.7,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"Diarrhoea","anyGradePct":18,"grade3PlusPct":0.3,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"Leukopenia","anyGradePct":17,"grade3PlusPct":3,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"Neutropenia","anyGradePct":16,"grade3PlusPct":5,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"MDS/AML","anyGradePct":1.2,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"Cumulative across trials; 54% fatal"},{"event":"Pneumonitis","anyGradePct":1,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"},{"event":"Venous thromboembolism (prostate)","anyGradePct":8,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=741ff3e3-dc1a-45a6-84e5-2481b27131aa","note":"OlympiA adjuvant, n=911"}],"access":[{"country":"US","reimbursement":"Medicare Part D (oral); commercial plans per formulary, often with prior authorisation","assistance":"https://www.astrazeneca-us.com/medicines/access-360","source":"https://www.cms.gov/medicare/payment/part-b-drugs/asp-pricing-files","asOf":"2026-09-06"},{"country":"UK","reimbursement":"NICE: recommended in ovarian maintenance (TA598, TA620), adjuvant gBRCA breast (TA886), metastatic breast (TA1100), prostate (TA887)","source":"https://www.nice.org.uk/guidance/published?ngt=Technology%20appraisal%20guidance","asOf":"2026-09-06"},{"country":"EU","reimbursement":"EMA approved across indications","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2014-12-19","type":"approval","region":"US","note":"gBRCA advanced ovarian cancer after ≥3 lines: first PARP inhibitor","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2017-08-17","type":"approval","region":"US","note":"Maintenance in platinum-sensitive recurrent ovarian cancer; tablet formulation","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2018-01-12","type":"approval","region":"US","note":"gBRCA HER2-negative metastatic breast cancer (OlympiAD)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2018-12-19","type":"approval","region":"US","note":"First-line maintenance in BRCA-mutated ovarian cancer (SOLO-1)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2019-12-27","type":"approval","region":"US","note":"gBRCA metastatic pancreatic cancer maintenance (POLO)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2020-05-19","type":"approval","region":"US","note":"HRR-mutant mCRPC (PROfound)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2022-03-11","type":"approval","region":"US","note":"Adjuvant gBRCA high-risk HER2-negative early breast cancer (OlympiA)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2023-05-31","type":"approval","region":"US","note":"With abiraterone in BRCA-mutated mCRPC (PROpel)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},{"id":"pasireotide","kind":"drug","name":"Pasireotide","aka":["SOM230"],"tldr":"Pasireotide is a second-generation somatostatin analogue that hits more receptor types than octreotide. It is approved for Cushing's disease and acromegaly caused by pituitary tumours when surgery has not cured them, at the cost of frequent high blood sugar.","summary":"Pasireotide (SOM230) was developed by Novartis and is now marketed by Recordati. The FDA approved the twice-daily subcutaneous form in 2012 for Cushing's disease when surgery is not an option or has failed, the first drug approved for that indication, and the monthly long-acting depot in 2014 for acromegaly inadequately controlled by surgery. It normalises cortisol in a minority and growth hormone and IGF-1 in a larger fraction of patients, and shrinks tumours in many.\n\nHyperglycaemia, from suppression of insulin and incretins, is the main side effect and often needs treatment. Beyond the pituitary, the phase 2 LUNA trial tested it alone and with everolimus in lung and thymic neuroendocrine tumours and found activity in each arm, without a placebo comparison. The pituitary tumours and lung neuroendocrine tumour pages name it.","status":"approved","asOf":"2026-09-17","wikipedia":"https://en.wikipedia.org/wiki/Pasireotide","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Pasireotide"}],"tags":["subtype-drugs-wave"],"related":["everolimus"],"indications":["lung-net"],"sections":[],"technologies":[],"targets":["sstr2"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Signifor / Signifor LAR","modality":"Multireceptor somatostatin analogue (subcutaneous or monthly depot)","mechanism":"Binds somatostatin receptors 1, 2, 3 and 5, with far higher affinity for SSTR5 than octreotide; SSTR5 dominates on corticotroph adenomas, so it suppresses ACTH in Cushing's disease and growth hormone in acromegaly resistant to first-generation analogues.","approvals":[{"region":"US","year":2012,"indication":"Cushing's disease when pituitary surgery is not an option or has not been curative"},{"region":"US","year":2014,"indication":"Acromegaly inadequately controlled by surgery or for whom surgery is not an option (long-acting depot)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"pembrolizumab","kind":"drug","name":"Pembrolizumab","aka":[],"tldr":"Pembrolizumab is a PD-1 blocking antibody approved in more than 40 settings, from melanoma and lung cancer to the first tumour-agnostic approval for mismatch-repair-deficient tumours in 2017, and before and after surgery in triple-negative breast cancer. A subcutaneous form arrived in 2025, and it is the backbone partner for ADCs and personalised neoantigen vaccines.","summary":"Approvals span melanoma, NSCLC, head and neck, Hodgkin, urothelial, MSI-H/dMMR tumours (first tumour-agnostic approval, 2017), gastric, oesophageal, cervical, HCC, RCC, endometrial, TNBC (KEYNOTE-355 metastatic CPS ≥10; KEYNOTE-522 neoadjuvant/adjuvant with 7-year OS benefit), TMB-high, and more. 2026 additions include platinum-resistant PD-L1+ ovarian cancer, adjuvant RCC with belzutifan, and combination labels with sacituzumab govitecan (ASCENT-04) and enfortumab vedotin. Subcutaneous Keytruda Qlex approved 2025. Backbone for neoantigen vaccines (intismeran).","status":"approved","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Pembrolizumab","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Pembrolizumab"}],"tags":[],"related":[],"indications":["hcc","rcc"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["merck"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Keytruda / Keytruda Qlex (SC)","modality":"Monoclonal antibody (anti-PD-1)","mechanism":"Humanised IgG4 blocking PD-1; restores T-cell effector function.","approvals":[{"region":"US","year":2014,"indication":"Melanoma (first of >40 indications)"},{"region":"US","year":2017,"indication":"MSI-H/dMMR solid tumours (tumour-agnostic)"},{"region":"US","year":2020,"indication":"Metastatic TNBC, PD-L1 CPS ≥10, with chemotherapy"},{"region":"US","year":2021,"indication":"High-risk early TNBC, neoadjuvant + adjuvant (KEYNOTE-522)"},{"region":"US","year":2026,"indication":"Platinum-resistant PD-L1+ ovarian cancer; adjuvant RCC with belzutifan; with sacituzumab govitecan in 1L TNBC"}],"mechanismSteps":["Antibody binds PD-1 on T cells","PD-1/PD-L1 engagement between T cell and tumour is blocked","Exhausted tumour-reactive T cells regain effector function","Interferon-γ and cytotoxic granules are released at the tumour","Tumour cells are killed; memory T cells persist"],"dosing":{"route":"IV infusion over 30 min (subcutaneous Keytruda Qlex available)","schedule":"200 mg every 3 weeks or 400 mg every 6 weeks; paediatric 2 mg/kg (max 200 mg) every 3 weeks; up to 24 months in most metastatic settings","modifications":"Hold for grade 2 immune-mediated events; permanently discontinue for grade 4 or recurrent grade 3","monitoring":"Thyroid function, LFTs, creatinine, glucose at baseline and periodically; patient education on immune-related symptoms","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287"},"toxicity":[{"event":"Hypothyroidism (immune-mediated)","anyGradePct":8,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Pneumonitis (immune-mediated)","anyGradePct":3.4,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Colitis (immune-mediated)","anyGradePct":1.7,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Hepatitis (immune-mediated)","anyGradePct":0.7,"source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Fatigue","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Musculoskeletal pain","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Rash","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Diarrhoea","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"},{"event":"Pyrexia","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9333c79b-d487-4538-a9f0-71b91a02b287","note":"Pooled monotherapy data, >2,800 patients"}],"access":[{"country":"US","listPrice":"$11,564 per 200 mg dose (WAC, Merck price disclosure 2024)","reimbursement":"Medicare Part B (physician-administered); commercial plans per formulary","assistance":"https://www.merckaccessprogram-keytruda.com","source":"https://www.cms.gov/medicare/payment/part-b-drugs/asp-pricing-files","asOf":"2026-09-06"},{"country":"UK","reimbursement":"NICE: recommended across many indications (melanoma, NSCLC, TNBC KEYNOTE-522/355, RCC, HNSCC, cervical, oesophageal and others)","source":"https://www.nice.org.uk/guidance/published?ngt=Technology%20appraisal%20guidance","asOf":"2026-09-06"},{"country":"EU","reimbursement":"EMA approved; reimbursed in all member states for core indications","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2014-09-04","type":"approval","region":"US","note":"Accelerated approval, advanced melanoma after ipilimumab; first PD-1 inhibitor in the US","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2015-10-02","type":"approval","region":"US","note":"PD-L1+ NSCLC after platinum","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2017-05-23","type":"approval","region":"US","note":"MSI-H/dMMR solid tumours: first tumour-agnostic approval","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2020-06-16","type":"approval","region":"US","note":"TMB-high solid tumours (tumour-agnostic)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2020-11-13","type":"approval","region":"US","note":"Metastatic TNBC, PD-L1 CPS ≥10, with chemotherapy (KEYNOTE-355)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2021-07-26","type":"approval","region":"US","note":"High-risk early TNBC, neoadjuvant and adjuvant (KEYNOTE-522)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2023-10-16","type":"approval","region":"US","note":"Perioperative NSCLC (KEYNOTE-671)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2025-09","type":"approval","region":"US","note":"Subcutaneous pembrolizumab (Keytruda Qlex)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2026-Q1","type":"approval","region":"US","note":"Platinum-resistant PD-L1+ ovarian cancer","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2026-06-12","type":"approval","region":"US","note":"Adjuvant RCC with belzutifan (LITESPARK-022)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-belzutifan-pembrolizumab-adjuvant-treatment-renal-cell-carcinoma"},{"date":"2026-06-24","type":"approval","region":"US","note":"First-line PD-L1+ TNBC with sacituzumab govitecan (ASCENT-04)","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-sacituzumab-govitecan-hziy-monotherapy-and-combination-pembrolizumab-first-line"},{"date":"2026-07-10","type":"approval","region":"US","note":"Muscle-invasive bladder cancer with enfortumab vedotin, as pembrolizumab or pembrolizumab with berahyaluronidase alfa","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-pembrolizumab-or-pembrolizumab-and-berahyaluronidase-alfa-pmph-each-enfortumab-vedotin"}]},{"id":"phosphorus-32","kind":"drug","name":"Phosphorus-32 (radiophosphorus)","aka":["Radiophosphorus","Sodium phosphate P-32","32P"],"tldr":"Radiophosphorus was one of the first treatments for polycythaemia vera, from the 1940s: a radioactive phosphate injection that quietened the overactive bone marrow for a year or more. It was abandoned when trials showed it raised the risk of leukaemia.","summary":"Phosphorus-32 was introduced by John Lawrence at Berkeley in the late 1930s as the first therapeutic use of an artificial radionuclide, and became a standard treatment for polycythaemia vera and essential thrombocythaemia. A single intravenous dose controlled blood counts for one to two years and was convenient for older patients.\n\nThe Polycythemia Vera Study Group's first randomised trial, launched in 1967, compared phlebotomy alone, phlebotomy plus radiophosphorus and phlebotomy plus chlorambucil, and showed that both radiophosphorus and chlorambucil raised the risk of acute leukaemia several-fold. Radiophosphorus was thereafter restricted to the very elderly and is now rarely used, replaced by hydroxyurea, interferon and JAK inhibitors. The polycythaemia vera page records it in the history of the disease.","status":"historic","asOf":"2026-09-17","wikipedia":"https://en.wikipedia.org/wiki/Phosphorus-32","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Phosphorus-32"}],"tags":["subtype-drugs-wave"],"related":["p-32"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"Intravenous radiopharmaceutical (beta emitter; historic)","mechanism":"Phosphate labelled with the beta emitter phosphorus-32 is taken up by rapidly dividing marrow cells and incorporated into their DNA, where the radiation suppresses the overactive marrow of polycythaemia vera.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"pylarify","kind":"drug","name":"Piflufolastat F-18 / Pylarify TruVu","aka":[],"tldr":"Piflufolastat F-18 (Pylarify) is the leading PSMA PET tracer for prostate cancer, with a new formulation approved in March 2026.","summary":"Piflufolastat F-18 is a PET tracer: an 18F-labelled urea that binds prostate-specific membrane antigen (PSMA), lighting up prostate cancer deposits that conventional CT and bone scan miss. It was approved in 2021 for PSMA PET in initial staging and biochemical recurrence, and Lantheus' Pylarify TruVu formulation, approved on 9 March 2026, offers an improved formulation and distribution profile. A single 333 MBq dose is injected and imaging follows 60 to 120 minutes later; adverse effects are minor. The 18F label allows central manufacture and shipping, unlike generator-produced 68Ga agents, and it competes with Illuccix/Gozellix (68Ga, Telix), Locametz (Novartis) and Posluma. The open question is whether the management changes PSMA PET triggers translate into longer survival. For a newcomer: the leading tracer for seeing where prostate cancer actually is.","status":"approved","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/Piflufolastat_F-18","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Piflufolastat%20F-18"}],"tags":[],"related":["f-18","ga-68"],"indications":["prostate"],"sections":[],"technologies":["psma-pet"],"targets":["psma"],"drugs":[],"companies":["lantheus"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Pylarify","code":"18F-DCFPyL","modality":"PET imaging agent","mechanism":"18F-labelled PSMA-binding urea.","approvals":[{"region":"US","year":2021,"indication":"PSMA PET imaging in prostate cancer"},{"region":"US","year":2026,"indication":"Pylarify TruVu formulation"},{"region":"EU","year":2023,"indication":"EU brand Pylclari (Curium)"}],"mechanismSteps":["18F-labelled small molecule binds the PSMA active site","Tracer is internalised and retained in prostate cancer cells","Positron emissions are detected by the PET scanner","Whole-body map of PSMA-expressing disease is produced","Result selects patients for PSMA radioligand therapy"],"dosing":{"route":"IV injection (diagnostic)","schedule":"333 MBq (9 mCi) single dose; imaging 60-120 minutes later","monitoring":"Hydration and voiding to reduce bladder dose","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},"toxicity":[{"event":"Headache","note":"Rare; diagnostic dose"},{"event":"Dysgeusia"},{"event":"Fatigue"}],"access":[{"country":"US","reimbursement":"Medicare pass-through/payment for PSMA PET; broad commercial coverage for staging and biochemical recurrence","source":"https://www.cms.gov/medicare/payment/part-b-drugs/asp-pricing-files","asOf":"2026-09-06"}],"regulatoryEvents":[{"date":"2021-05-26","type":"approval","region":"US","note":"PSMA PET imaging in prostate cancer: first 18F PSMA agent","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"},{"date":"2026-03-09","type":"approval","region":"US","note":"Pylarify TruVu formulation","source":"https://www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications"}]},{"id":"psma-1007-f18","kind":"drug","name":"PSMA-1007 F-18","aka":["Prostalumin"],"tldr":"PSMA-1007 is a fluorine-18 PSMA PET tracer from ABX in Germany, widely used in Europe for prostate cancer staging because little of it reaches the bladder, and in a phase 3 trial registered by its maker.","summary":"PSMA-1007, developed at Heidelberg and manufactured by ABX advanced biochemical compounds in Radeberg, is a fluorine-18 PSMA ligand whose low urinary excretion improves views of the prostate bed and pelvic nodes. It is authorised in several European countries and Canada and used in many centres alongside gallium-68 PSMA-11 and piflufolastat; a phase 3 trial by ABX is registered on ClinicalTrials.gov. Health Canada's Drug Product Database lists PROSTALUMIN ((18F)PSMA-1007, 3.7 GBq/mL intravenous solution, DIN 02571757) from the Centre for Probe Development and Commercialization in Hamilton, Ontario, with status Approved and a product monograph dated 24 September 2026.","status":"phase-3","asOf":"2026-10-04","links":[{"label":"ClinicalTrials.gov: trials of PSMA-1007 F-18","url":"https://clinicaltrials.gov/search?intr=PSMA-1007%20F-18"},{"label":"Health Canada Drug Product Database: PROSTALUMIN, DIN 02571757","url":"https://health-products.canada.ca/dpd-bdpp/info?lang=eng&code=107378"}],"tags":["pipeline","ctgov-ingest"],"related":["f-18","ga-68"],"indications":["prostate"],"sections":[],"technologies":["psma-pet","pet"],"targets":["psma"],"drugs":[],"companies":["abx-advanced-biochemical-compounds"],"institutions":[],"pathways":[],"terms":[],"trials":["nct06122584"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2, curated)","editedOn":"2026-09-16"},"modality":"PSMA-targeted PET radiotracer, fluorine-18","mechanism":"A fluorine-18 PSMA ligand excreted mainly through the liver rather than the kidneys, so the bladder does not obscure the prostate bed on PET.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"radioactive-iodine","kind":"drug","name":"Radioactive iodine (I-131)","aka":[],"tldr":"The original targeted radiotherapy: thyroid cells soak up iodine, so radioactive iodine destroys leftover thyroid tissue and metastases while sparing everything else.","summary":"In use since 1946 for differentiated thyroid cancer; the archetype of theranostics (I-123 or I-131 scans image the same uptake). Roles: remnant ablation after thyroidectomy (now omitted in low-risk disease after ESTIMABL2, IoN, HiLo), adjuvant treatment of intermediate/high-risk disease, and treatment of iodine-avid metastases. Given after TSH stimulation (withdrawal or recombinant TSH). Salivary damage, secondary malignancy at high cumulative doses, and refractoriness in dedifferentiated tumours are the limits.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Iodine-131","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Radioactive%20iodine"}],"tags":[],"related":["i-123","i-131"],"indications":["thyroid"],"sections":[],"technologies":["radioiodine-therapy","radioligand-therapy"],"targets":["sstr2"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":["theranostics","radioiodine-term"],"trials":["hilo","estimabl2","ion-trial"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Sodium iodide I-131","modality":"Radiopharmaceutical (beta/gamma emitter, natural uptake)","mechanism":"Sodium-iodide symporter (NIS) concentrates iodide in thyroid follicular cells; I-131 beta particles (mean path ~0.8 mm) irradiate the cell and neighbours; gamma emission enables imaging.","approvals":[{"region":"US","year":1951,"indication":"Hyperthyroidism and thyroid carcinoma (first radiopharmaceutical approval)"}],"mechanismSteps":["TSH stimulation upregulates the sodium-iodide symporter on thyroid cells","Oral I-131 is absorbed and concentrated in thyroid tissue and iodine-avid metastases","Beta decay deposits radiation within ~1 mm, killing the cells over weeks","Gamma emission allows a post-therapy scan to map uptake"],"dosing":{"route":"Oral capsule or solution","schedule":"1.1 GBq (30 mCi) for remnant ablation (HiLo); 3.7-7.4 GBq for adjuvant or metastatic treatment; low-iodine diet and TSH stimulation beforehand","monitoring":"Post-therapy whole-body scan; thyroglobulin; salivary and marrow function","source":"https://www.thyroid.org/professionals/ata-professional-guidelines/"},"toxicity":[{"event":"Sialadenitis / xerostomia","source":"https://www.thyroid.org/professionals/ata-professional-guidelines/","note":"Dose-dependent; common after repeated high-activity treatment"}],"access":[],"regulatoryEvents":[{"date":"1946","type":"approval","region":"US","note":"First therapeutic use in thyroid cancer (Seidlin); formal approval followed"}]},{"id":"radium-223","kind":"drug","name":"Radium-223 dichloride","aka":[],"tldr":"Radium-223 was the first alpha-emitting drug ever approved (2013). It homes to bone like calcium and treats prostate cancer that has spread only to bone.","summary":"Radium-223 is a calcium mimetic incorporated into bone matrix at sites of metastatic bone turnover, where each decay chain delivers four alpha emissions over a range of a few cells, killing tumour while largely sparing marrow. It is given intravenously to men with symptomatic castration-resistant prostate cancer whose spread is confined to bone without visceral disease. ALSYMPCA showed overall survival of 14.9 versus 11.3 months (HR 0.70) and fewer skeletal events, and it became the first alpha-emitting drug ever approved (2013). ERA 223 showed excess fractures when combined with abiraterone, now contraindicated without bone protection, while PEACE III (2024) with enzalutamide plus bone-protecting agents was positive for rPFS and overall survival. How to sequence it with 177Lu-PSMA therapy is unresolved. Simply put, it is a radioactive calcium look-alike that homes to bone metastases.","status":"approved","asOf":"2026-09-06","wikipedia":"https://en.wikipedia.org/wiki/Radium-223","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Radium-223%20dichloride"}],"tags":[],"related":["lu-177","ra-223"],"indications":["prostate","prostate-mcrpc"],"sections":[],"technologies":["targeted-alpha-therapy"],"targets":[],"drugs":[],"companies":["bayer"],"institutions":[],"pathways":[],"terms":["alpha-vs-beta"],"trials":["alsympca"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Xofigo","modality":"Targeted alpha therapy (bone-seeking)","mechanism":"Calcium mimetic incorporated into bone matrix at metastases; four alpha emissions per decay chain.","approvals":[{"region":"US","year":2013,"indication":"Symptomatic bone-metastatic CRPC without visceral disease"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"re-188-sct","kind":"drug","name":"Rhenium-188 skin cancer therapy","aka":["Rhenium-SCT","188Re epidermal radionuclide therapy"],"tldr":"A radioactive paste is spread over a thin film placed on top of a skin cancer. The radiation only travels a few millimetres, so it treats the visible tumour without surgery, cutting, or affecting deeper tissue.","summary":"Rhenium-SCT (Skin Cancer Therapy) is a non-invasive, single-session epidermal brachytherapy for non-melanoma skin cancer (basal cell carcinoma and cutaneous squamous cell carcinoma), developed by OncoBeta. Rhenium-188 (half-life about 17 hours) is produced on demand from a tungsten-188/rhenium-188 generator and formulated as a resin that is applied to an adhesive foil placed over the lesion, so the radioactive material never directly contacts the skin. A typical prescribed dose is 50 Gy to the deepest point of the lesion (target depth up to about 3 mm).\n\nThe device and compound are registered in Australia (ARTG, class IIb, from 2020-2022) and hold CE marking, with use reported across Europe, the UK, New Zealand and South Africa; it does not have FDA approval. A single-arm, multicentre phase 4 post-marketing study (EPIC-Skin) reported, at 12 months, lesion-based complete response in 94.1% and partial response in 3.2% of 185 evaluable lesions, with no toxicities above CTCAE grade 2 and favourable cosmetic and quality-of-life outcomes; an earlier Italian series (Castellucci et al., EJNMMI Physics) reported 98% complete lesion response at 6 months in 54 evaluable lesions.\n\nBecause treatment is external and the isotope's beta range is only a few millimetres, Rhenium-SCT is positioned for lesions ≤3 mm deep and ≤8 cm2 in difficult-to-treat cosmetic or functional sites (nose, ear, lip, digits, genitals) where surgery or conventional external-beam radiotherapy is less attractive.","status":"approved","asOf":"2026-09-22","links":[{"label":"OncoBeta: Rhenium-SCT technology overview","url":"https://www.oncobeta.com/technology/"},{"label":"EPIC-Skin phase 4 study, 12-month results (PMC, 2025)","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC12197855/"},{"label":"Castellucci et al., high-dose brachytherapy with non-sealed 188Re for non-melanoma skin cancer, EJNMMI","url":"https://www.healthcert.com/hubfs/EJNMMI%20Castellucci%20-%20Savoia%20et%20al.%202020.pdf"},{"label":"Australian MSAC public summary document on Rhenium-188 brachytherapy for skin cancer","url":"https://www.msac.gov.au/sites/default/files/2025-07/1657.1_final_psd_-_april_2025_-_redacted.pdf"}],"tags":["brachytherapy","skin cancer","beta emitter","non-invasive"],"related":["re-188"],"indications":[],"sections":[],"technologies":["ldr-seed-brachytherapy"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Rhenium-SCT","modality":"brachytherapy source","mechanism":"A resin containing the beta- and gamma-emitting radioisotope rhenium-188 is applied directly to the skin over a thin protective foil moulded to the shape of a non-melanoma skin lesion. Beta particles penetrate only a few millimetres, delivering a high local dose to the tumour (about 92% of the dose within 2 mm) while a single outpatient application typically lasts under an hour.","approvals":[{"region":"EU/UK/AU/NZ/ZA","year":2015,"indication":"Shallow (≤3 mm deep) basal cell carcinoma and squamous cell carcinoma without perineural invasion or high-risk pathology","note":"CE marking and national device registrations; not FDA approved"}],"mechanismSteps":[],"dosing":{"route":"Topical epidermal application (resin on adhesive foil placed over the lesion)","schedule":"Single outpatient session, typically prescribing 50 Gy to the deepest point of the lesion","source":"https://pmc.ncbi.nlm.nih.gov/articles/PMC12197855/"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"rituximab","kind":"drug","name":"Rituximab","aka":["Rituximab and Hyaluronidase Human","Rituxan Hycela"],"tldr":"Rituximab was the first antibody ever approved for cancer (1997). It made chemoimmunotherapy the CLL standard for a decade, and biosimilars keep it cheap and everywhere.","summary":"Approved in follicular lymphoma (1997), DLBCL (2006, R-CHOP), CLL (2010, with fludarabine-cyclophosphamide: FCR, the first regimen to show OS benefit in CLL). Superseded in CLL by targeted agents (CLL13, CLL14, ELEVATE-TN) but still used with venetoclax in relapse (MURANO: venetoclax-rituximab 24 months) and in resource-limited settings. Biosimilars (Truxima, Ruxience, Riabni) since 2018.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Rituximab","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Rituximab"}],"tags":[],"related":[],"indications":["dlbcl"],"sections":[],"technologies":[],"targets":["cd20"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Rituxan / MabThera (and biosimilars)","modality":"Monoclonal antibody (anti-CD20, chimeric)","mechanism":"Chimeric type I anti-CD20 IgG1: CDC, ADCC, and modest direct signalling.","approvals":[{"region":"US","year":1997,"indication":"Relapsed follicular lymphoma; first antibody approved for cancer"},{"region":"US","year":2010,"indication":"CLL with fludarabine and cyclophosphamide"}],"mechanismSteps":["Binds CD20 and clusters it into lipid rafts","Complement is fixed (CDC) and NK cells recruited (ADCC)","B cells and CLL cells are lysed; normal B cells recover after 6-12 months"],"dosing":{"route":"IV or subcutaneous (Rituxan Hycela)","schedule":"CLL: 375 mg/m² cycle 1 then 500 mg/m² cycles 2-6 with chemotherapy or venetoclax","monitoring":"Infusion reactions, HBV reactivation (boxed), PML (boxed), late-onset neutropenia","source":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Rituxan"},"toxicity":[{"event":"Infusion-related reactions (first infusion)","anyGradePct":77,"source":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Rituxan","note":"Historic lymphoma data; lower with premedication"},{"event":"Hepatitis B reactivation","note":"Boxed warning; screen all patients"},{"event":"Late-onset neutropenia","anyGradePct":8}],"access":[],"regulatoryEvents":[]},{"id":"rb-82-chloride","kind":"drug","name":"Rubidium Rb-82 chloride","aka":["Rb-82","82Rb"],"tldr":"A generator-produced radioactive form of the metal rubidium, chemically similar to potassium, given as a fast intravenous infusion; because it decays away in about a minute and a half it can be produced on site without a cyclotron, letting a PET scan of heart blood flow be done in around half an hour.","summary":"Rubidium Rb-82 chloride, marketed via the CardioGen-82 strontium-82/rubidium-82 generator, is a PET myocardial perfusion agent behaving like a potassium analogue with a first-pass extraction fraction of about 65% (and flow-dependent roll-off similar to or greater than the Tc-99m SPECT agents). Its ultra-short 75-second half-life is both its main practical advantage, no cyclotron is required since the generator is eluted with saline immediately before each dose, and its main constraint: imaging must begin within 60-130 seconds of infusion and the generator itself is regulated for strontium breakthrough.\n\nThe FDA label indicates it for PET imaging of the myocardium under rest or pharmacologic stress to evaluate regional myocardial perfusion in adults with suspected or existing coronary artery disease. Recommended adult dosing (Model 510 infusion system) is 1,480 MBq (40 mCi) per rest or stress component, with a range of 1,110-2,220 MBq, infused intravenously at 50 mL/min; a newer Model 1700 system doses by body weight (10-30 MBq/kg).\n\nRb-82 PET's speed (a full rest/stress study in about 30 minutes) and generator-based, cyclotron-free production have made it the most widely used PET perfusion tracer in the US for routine CAD work-up, and it is also used, alongside or instead of N-13 ammonia, as the resting perfusion half of the cardiac sarcoidosis PET protocol.","asOf":"2026-09-22","links":[{"label":"FDA label: CardioGen-82 (rubidium Rb 82 generator), 2024 revision","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/019414s034lbl.pdf"},{"label":"EMC SmPC: Cardiogen-82 (Rb-82 extraction fraction 65%)","url":"https://www.medicines.org.uk/emc/product/15771/smpc"},{"label":"ASNC/SNMMI PET nuclear cardiology procedure standard","url":"https://www.asnc.org/wp-content/uploads/2024/06/s12350-016-0522-3.pdf"}],"tags":["PET","myocardial perfusion","generator"],"related":["n-13-ammonia","f-18-flurpiridaz","tc-99m","n-13","rb-82"],"indications":["coronary-artery-disease","cardiac-sarcoidosis"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"CardioGen-82","modality":"PET tracer","mechanism":"Rb+ is a potassium analogue taken up by viable myocytes through the Na+/K+-ATPase pump, similarly to thallium, with a first-pass myocardial extraction fraction of about 65% at rest that falls further at high flow (roughly 40-70% across the physiological range, per comparative reviews), a bigger flow-dependent roll-off than the newer tracer flurpiridaz. Its 75-second physical half-life means it is produced on demand from a strontium-82/rubidium-82 generator immediately before each rest and stress dose, with no cyclotron needed on site, but also that imaging must start within roughly a minute of the infusion and the whole rest-stress study can be completed in about 30 minutes.","approvals":[{"region":"US","year":1989,"indication":"PET imaging of the myocardium under rest or pharmacologic stress to evaluate regional myocardial perfusion in adults with suspected or existing coronary artery disease"}],"mechanismSteps":[],"dosing":{"route":"Intravenous infusion (generator-eluted, produced immediately before use)","schedule":"1,480 MBq (40 mCi) per rest or stress component, range 1,110-2,220 MBq, infused at 50 mL/min (Model 510); 10-30 MBq/kg on Model 1700; imaging starts 60-90 seconds after infusion, rest and stress separated by a minimum 10 minutes","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/019414s034lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"samarium-153-lexidronam","kind":"drug","name":"Samarium-153 lexidronam","aka":["153Sm-EDTMP","Samarium Sm 153 lexidronam pentasodium"],"tldr":"Quadramet (samarium-153 lexidronam) is a radioactive bone-seeking injection that lodges in bone metastases and irradiates them from inside, approved in 1997 to relieve pain from prostate, breast and other cancers spread to bone. Most patients get relief within one to two weeks, but marrow suppression follows at three to five weeks, and radium-223 and PSMA radioligands have largely replaced it.","summary":"Samarium-153 lexidronam was approved by the FDA in March 1997 and authorised in the EU in February 1998 for relief of pain in patients with confirmed osteoblastic metastatic bone lesions that take up technetium-labelled bisphosphonate on bone scan, on placebo-controlled trials in which most patients had pain relief within one to two weeks lasting for months. It and strontium-89 (Metastron) were the bone-pain radiopharmaceuticals of the 1990s; radium-223 (Xofigo), which extends survival in prostate cancer, and PSMA radioligands have since taken most of their role. A single intravenous dose is given; transient marrow suppression, with nadir at three to five weeks, is the main toxicity, and a pain flare can occur early. Distributed by Lantheus in the US and Curium in Europe.","status":"approved","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Samarium_(153Sm)_lexidronam","links":[{"label":"EPAR (EMA)","url":"https://www.ema.europa.eu/en/medicines/human/EPAR/quadramet"},{"label":"US label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=samarium"}],"tags":["ema-list","supportive"],"related":["radium-223","ra-223","sm-153","sr-89"],"indications":["prostate"],"sections":[],"technologies":["radioligand-therapy"],"targets":[],"drugs":[],"companies":["lantheus","curium"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Quadramet","modality":"Bone-seeking therapeutic radiopharmaceutical (beta emitter)","mechanism":"Samarium-153 chelated to the tetraphosphonate EDTMP concentrates in areas of high bone turnover around osteoblastic metastases; beta emission (1.9 day half-life) irradiates the metastases and relieves pain, with gamma emission allowing imaging.","approvals":[{"region":"US","year":1997,"indication":"Relief of pain in patients with confirmed osteoblastic metastatic bone lesions that enhance on radionuclide bone scan"},{"region":"EU","year":1998,"indication":"Relief of bone pain from multiple painful osteoblastic skeletal metastases (Quadramet)"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"f-18-naf","kind":"drug","name":"Sodium fluoride F-18","aka":["18F-NaF","Na18F","Fluoride F-18"],"tldr":"A radioactive form of fluoride that collects in areas of bone rebuilding. A PET scan after the injection shows those hot spots, which can be cancer that has spread to bone or something harmless like a healed fracture.","summary":"Sodium fluoride F-18 is one of the oldest PET radiopharmaceuticals: it was first approved by FDA in 1972 (NDA 17-042, held by the predecessor of GE Healthcare) as a bone-imaging agent, then re-approved under a newer label format in 2011 (NDA 22-494, sponsor National Cancer Institute) after the original product had lapsed commercially. Both approvals cover PET imaging of bone to define areas of altered osteogenic activity; neither approval is oncology-specific, but the agent's principal modern use is detecting osteoblastic bone metastases, most often from prostate and breast cancer, where it offers higher sensitivity and better spatial resolution than technetium-99m bone scintigraphy.\n\nThe recommended adult dose is 300-450 MBq (8-12 mCi) intravenously, with imaging optimally at one to two hours; no adverse reactions have been established in the FDA label, and the main safety statement concerns cumulative radiation exposure rather than a pharmacological toxicity. Because uptake is a marker of bone turnover, not malignancy, degenerative disease, fracture healing and other benign remodelling can be false positives, and correlation with CT or MRI is standard practice.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Sodium Fluoride F 18 Injection (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d867a881-108e-41fa-91ab-dc4df00cbb55"},{"label":"FDA approval letter, NDA 22-494 (2011)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022494Orig1s000Approv.pdf"}],"tags":["bone imaging","PET","generic"],"related":["f-18","tc-99m"],"indications":["prostate"],"sections":[],"technologies":["pet","pet-ct"],"targets":[],"drugs":[],"companies":["ge-healthcare"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"PET tracer","mechanism":"Fluoride ion exchanges with hydroxyl groups on the hydroxyapatite crystal surface of bone, concentrating wherever bone turnover (osteoblastic activity) is high. Uptake reflects blood flow and new bone formation rather than tumour cells directly, so it lights up both malignant and benign remodelling.","approvals":[{"region":"US","year":1972,"indication":"Diagnostic PET imaging of bone to define areas of altered osteogenic activity (NDA 17-042)"},{"region":"US","year":2011,"indication":"Diagnostic PET imaging of bone to define areas of altered osteogenic activity (NDA 22-494, current labelling)"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"300-450 MBq (8-12 mCi) in adults; imaging can begin 1-2 hours after administration, optimally at one hour","source":"https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d867a881-108e-41fa-91ab-dc4df00cbb55"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"sorafenib","kind":"drug","name":"Sorafenib","aka":[],"tldr":"The first drug ever to extend life in advanced liver cancer (2007), now mostly a comparator arm that newer combinations are measured against.","summary":"SHARP: OS 10.7 vs 7.9 months versus placebo (HR 0.69). Standard first-line therapy for a decade until REFLECT (lenvatinib non-inferior) and IMbrave150 (atezolizumab-bevacizumab superior). Also approved in RCC and radioiodine-refractory thyroid cancer. Hand-foot skin reaction and diarrhoea dominate toxicity.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Sorafenib","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Sorafenib"}],"tags":[],"related":[],"indications":["hcc","rcc","thyroid"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["bayer"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Nexavar","modality":"Small-molecule multi-kinase inhibitor (VEGFR, PDGFR, RAF)","mechanism":"Oral inhibitor of VEGFR1-3, PDGFR-β, KIT, FLT3 and RAF kinases; anti-angiogenic and anti-proliferative.","approvals":[{"region":"US","year":2005,"indication":"Advanced RCC"},{"region":"US","year":2007,"indication":"Unresectable HCC"},{"region":"US","year":2013,"indication":"Radioiodine-refractory differentiated thyroid cancer"}],"mechanismSteps":["Enters tumour and endothelial cells","Blocks VEGFR/PDGFR signalling in vessels, cutting blood supply","Inhibits RAF-MEK-ERK in tumour cells","Tumour growth slows; rarely shrinks"],"dosing":{"route":"Oral","schedule":"400 mg twice daily continuously","modifications":"Dose reduction to 400 mg daily for grade 2-3 hand-foot skin reaction","monitoring":"Blood pressure, skin, liver function"},"toxicity":[{"event":"Diarrhoea","anyGradePct":39,"grade3PlusPct":8,"note":"SHARP"},{"event":"Hand-foot skin reaction","anyGradePct":21,"grade3PlusPct":8,"note":"SHARP"},{"event":"Fatigue","anyGradePct":22,"grade3PlusPct":4,"note":"SHARP"}],"access":[],"regulatoryEvents":[{"date":"2007-11-16","type":"approval","region":"US","note":"Unresectable HCC on SHARP"}]},{"id":"sr-89-chloride","kind":"drug","name":"Strontium-89 chloride","aka":["Metastron","Strontium89","89SrCl2"],"tldr":"A radioactive form of strontium is injected into a vein. Because it behaves like calcium, it collects in the damaged, overactive bone around cancer that has spread to bone, and its radiation can relieve bone pain for months.","summary":"Strontium-89 chloride (branded Metastron) is indicated for the relief of bone pain in patients with painful skeletal metastases, confirmed by a prior bone scan; it is not a treatment for the underlying cancer and does not relieve pain from soft tissue disease. The FDA label recommends a fixed dose of 148 MBq (4 mCi) by slow intravenous injection over one to two minutes, or a weight-based alternative of 1.5-2.2 MBq/kg (40-60 microCi/kg); repeat dosing is generally not recommended at intervals of less than 90 days and depends on haematological recovery.\n\nStrontium-89 decays by beta emission with a physical half-life of 50.5 days; roughly two-thirds of excretion is urinary and one-third faecal in patients with bone metastases, with retention in metastatic lesions lasting much longer than the roughly 14-day turnover in normal bone. Pain relief typically begins 10-20 days after injection and can last three to six months; a transient pain flare in the first few days is common.\n\nMetastron was originally marketed by Amersham/Zeneca and later GE Healthcare; the branded product was discontinued and the compound is now supplied generically (marketed as Strontium89). It sits alongside samarium-153 lexidronam and radium-223 dichloride as FDA/EMA-approved bone-palliation radiopharmaceuticals, though 89Sr and 153Sm are not tumour-type-restricted the way radium-223's label is limited to castration-resistant prostate cancer.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Metastron (strontium-89 chloride injection)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020134s012lbl.pdf"},{"label":"SNMMI/EANM procedure guideline for palliative radionuclide bone therapies, 2023","url":"https://tech.snmjournals.org/content/51/3/176"}],"tags":["bone pain palliation","beta emitter","calcium mimetic"],"related":["radium-223","samarium-153-lexidronam","bone-metastases","ra-223","sm-153","sr-89"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Metastron","modality":"radioligand therapy","mechanism":"Strontium-89 chloride is a calcium-mimetic, bone-seeking beta emitter given by intravenous injection. It behaves like calcium, clearing from blood and localising preferentially in bone mineral at sites of active osteogenesis, so blastic metastatic lesions accumulate far more strontium than normal bone and receive a higher local radiation dose that palliates pain.","approvals":[{"region":"US","year":1993,"indication":"Relief of bone pain in patients with painful skeletal metastases (presence of bone metastases must be confirmed prior to therapy)"}],"mechanismSteps":[],"dosing":{"route":"Slow intravenous injection (1-2 minutes)","schedule":"148 MBq (4 mCi) fixed dose, or 1.5-2.2 MBq/kg (40-60 microCi/kg); repeat doses generally not within 90 days, based on response and haematological status","monitoring":"Blood counts (platelets, neutrophils) before and after treatment; confirm blastic bone metastases on bone scan before therapy","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020134s012lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"sunitinib","kind":"drug","name":"Sunitinib","aka":[],"tldr":"Sunitinib is an anti-angiogenic pill approved for pancreatic neuroendocrine tumours, kidney cancer and GIST.","summary":"Sunitinib is an oral inhibitor of VEGFR1-3, PDGFR, KIT, FLT3 and RET that blocks tumour blood-vessel growth and, in GIST, the KIT driver itself. It is approved for advanced renal cell carcinoma and imatinib-resistant GIST (2006), progressive pancreatic neuroendocrine tumours (2011, 37.5 mg daily continuously) and, little used, as adjuvant therapy in high-risk RCC (S-TRAC, 2017). The pancreatic NET phase 3 (Raymond 2011) showed PFS of 11.4 versus 5.5 months and was stopped early for benefit. In kidney cancer it has been largely displaced by immunotherapy combinations and is the control arm they beat in CheckMate 214, KEYNOTE-426, CheckMate 9ER and CLEAR, while it is still standard second line in GIST. Fatigue, diarrhoea, hand-foot syndrome, hypertension and hypothyroidism are common. For a newcomer, sunitinib defined first-line kidney cancer treatment before immunotherapy.","status":"approved","asOf":"2026-09-07","wikipedia":"https://en.wikipedia.org/wiki/Sunitinib","links":[{"label":"FDA label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Sunitinib"}],"tags":[],"related":[],"indications":["neuroendocrine","rcc","metastatic-ppgl"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["pfizer"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":["In kidney cancer: Motzer 2007 showed PFS 11 versus 5 months against interferon alfa and OS 26.4 versus 21.8 months, and sunitinib then served as the control arm of CheckMate 214, KEYNOTE-426, CheckMate 9ER and CLEAR; it is now mainly used in favourable-risk disease, where immunotherapy doublets show no OS gain, and in GIST, and has been generic since 2021. Resistance runs through alternative angiogenic pathways (FGF, MET, AXL)."],"brand":"Sutent","modality":"Small-molecule multi-kinase inhibitor (VEGFR, PDGFR, KIT)","mechanism":"Oral inhibitor of VEGFR1-3, PDGFR, KIT, FLT3, RET.","approvals":[{"region":"US","year":2006,"indication":"Advanced RCC; GIST after imatinib"},{"region":"US","year":2011,"indication":"Progressive pancreatic NETs"},{"region":"US","year":2017,"indication":"Adjuvant RCC at high risk (S-TRAC), little used"}],"mechanismSteps":[],"dosing":{"route":"Oral","schedule":"37.5 mg daily continuously (pNET)","monitoring":"Blood pressure, thyroid, cardiac function"},"toxicity":[{"event":"Diarrhoea","anyGradePct":59},{"event":"Nausea","anyGradePct":45},{"event":"Hypertension","anyGradePct":26,"grade3PlusPct":10},{"event":"Hand-foot syndrome","anyGradePct":23,"grade3PlusPct":6}],"access":[],"regulatoryEvents":[]},{"id":"technegas","kind":"drug","name":"Technegas (technetium Tc-99m labelled carbon inhalation aerosol)","aka":["Technegas","Tc-99m carbon nanoparticle aerosol","99mTc-CNP"],"tldr":"A puff of radioactive carbon particles so fine they travel with the breath into the depths of the lung, where they stick. A gamma camera then photographs which parts of the lung are getting air, which is compared with a second scan showing which parts are getting blood.","summary":"Technegas is an inhaled ventilation agent generated at the bedside: a Technegas generator flash-heats dried Tc-99m pertechnetate in a carbon crucible at roughly 2,700 C in argon, producing technetium encapsulated in carbon nanoparticle agglomerates measured at 60-160 nm, themselves built from 7-23 nm primary particles, with a radioactivity aerodynamic diameter below 500 nm. That size is the point: unlike a wet aerosol such as Tc-99m DTPA, which impacts in the central airways and gives hot spots in obstructive disease, Technegas distributes to the lung periphery and holds still long enough to image in multiple projections.\n\nThe FDA approved Technegas on 29 September 2023 under NDA 022335, held by Cyclomedica Australia, after decades of use elsewhere. The approved indication is narrow and precise: used with sodium pertechnetate Tc-99m in the Technegas Plus System, it is a radioactive diagnostic agent for adults and paediatric patients aged 6 years and older for visualisation of pulmonary ventilation and evaluation of pulmonary embolism when paired with perfusion imaging. Dosing is count-rate driven rather than fixed: 400-1,000 MBq (10.8-27 mCi) is loaded in the crucible to reach a lung count rate of 1,500-2,500 counts per second for adults, 500-1,000 for children, with inhalation completed within 10 minutes of preparation.\n\nThe US registration study, CYC-009 (NCT03054870), was a phase 3 non-inferiority comparison against xenon-133 planar ventilation imaging; its ClinicalTrials.gov record shows 226 participants actually enrolled and a terminated status. The label itself specifies imaging with a gamma camera and a low-energy collimator and does not use the words SPECT or planar, though the agent's stability in the lung is exactly what makes V/Q SPECT practical, and the EANM V/Q SPECT guideline is built around it.","status":"approved","asOf":"2026-09-23","links":[{"label":"FDA label: TECHNEGAS, kit for the preparation of technetium Tc 99m labeled carbon inhalation aerosol (NDA 022335)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/022335Orig1s000lbl.pdf"},{"label":"FDA approval package, NDA 022335, approval date 29 September 2023","url":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2024/022335Orig1s000Approv.pdf"},{"label":"Technegas particle characterisation: nanoparticle agglomerates of 60-160 nm (review)","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC10144982/"},{"label":"Cyclomedica: FDA grants approval for Technegas","url":"https://www.cyclomedica.com/2023/10/02/united-states-fda-grants-approval-for-technegas/"}],"tags":["ventilation","V/Q","technetium","inhaled"],"related":["tc-99m-maa","kr-81m","tc-99m","pulmonary-embolism-vq","cyclopharm","spect"],"indications":["pulmonary-embolism-vq"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":["nct03054870"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Technegas","modality":"Inhaled SPECT/gamma camera aerosol","mechanism":"Dried sodium pertechnetate Tc-99m is loaded into a graphite crucible and flash-heated to about 2,700 C for a few seconds in high-purity argon, which encapsulates the technetium inside carbon. The product is an ultrafine dispersion of carbon nanoparticle agglomerates with a radioactivity aerodynamic diameter under 500 nm, small enough to behave much like a gas: it follows inspired air to the alveoli rather than impacting in the large airways, then deposits and stays put, so the image is a map of where air actually reaches. Made with an argon/oxygen mix instead, the same generator yields Pertechnegas, whose technetium is not fully encased and which clears rapidly as soluble pertechnetate.","approvals":[{"region":"US","year":2023,"indication":"Visualisation of pulmonary ventilation, and evaluation of pulmonary embolism when paired with perfusion imaging, in adults and children aged 6 and over","note":"NDA 022335, Cyclomedica Australia, approved 29 September 2023"}],"mechanismSteps":[],"dosing":{"route":"Oral inhalation of the generated aerosol through a mouthpiece","schedule":"400-1,000 MBq (10.8-27 mCi) of Tc-99m pertechnetate loaded in the crucible for adults, inhaled by slow deep breathing with a 5-second breath-hold until a lung count rate of 1,500-2,500 counts per second is reached; 500-1,000 counts per second for children aged 6 and over. Inhalation must be completed within 10 minutes of preparation.","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/022335Orig1s000lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2023-09-29","type":"approval","region":"US","note":"FDA approval of NDA 022335 (Cyclomedica Australia), Type 3 new dosage form","source":"https://www.accessdata.fda.gov/drugsatfda_docs/nda/2024/022335Orig1s000Approv.pdf"}]},{"id":"pexiretide-tc99m","kind":"drug","name":"Technetium (99mTc) pexiretide","aka":["99mTc-3PRGD2","technetium [99mTc] pexiretide injection","Jilunte","3PRGD2","锝[99mTc]佩昔瑞特加肽注射液"],"tldr":"A Chinese-invented injection that makes tumours visible on the cheap, widely available type of scanner (SPECT) rather than the expensive one (PET). It was approved in China in April 2026 to check whether lung cancer has spread to the lymph nodes.","summary":"Pexiretide is a dimeric RGD peptide carrying three PEG spacers, labelled with technetium-99m, that targets integrin αvβ3 — a receptor expressed on new tumour blood vessels and on many tumour cells. It was developed by Professor Wang Fan's group at Peking University's Medical Isotope Research Centre on National Natural Science Foundation grants, and China's NMPA approved it on 2 April 2026 under the trade name Jilunte, for SPECT/CT assessment of regional lymph-node metastasis in patients with suspected lung cancer.\n\nThe funder's own announcement calls it the first Class 1 innovative radiopharmaceutical developed independently in China and the world's first broad-spectrum tumour imaging agent for SPECT — a claim about the modality, not the molecule: PET agents dominate general tumour imaging, while SPECT has been confined to bone, thyroid and perfusion work for decades. That distinction is the commercial point. China's installed base of SPECT/CT scanners is roughly two to three times its PET/CT base (Securities Times, citing industry estimates), and a SPECT scan costs a fraction of a PET scan, so a broad tumour agent that runs on the cheaper machine reaches district hospitals that will never own a cyclotron.\n\nThe registrational claim reported in Chinese coverage is that in phase 3 there was no statistically significant difference from 18F-FDG PET/CT in telling benign from malignant lung lesions, while for lung cancer lymph-node metastasis the specificity and accuracy of 99mTc-3PRGD2 SPECT/CT were significantly higher than PET/CT's. The trial report itself is not public in English; the closest peer-reviewed evidence is a prospective head-to-head study in 26 patients with primary malignant lung tumours (Korean Journal of Radiology, 2023), which compared the two scans across 42 metastatic and 136 benign lymph-node stations with histopathology as the reference.\n\nCommercially the agent sits with Ridio (Foshan), a company founded in 2012 out of the Peking University group, whose controlling shareholder is Beijing Jilunte Pharmaceutical; Baiyang Pharmaceutical invested in 2022 and holds the mainland commercialisation rights. An earlier filing was withdrawn in February 2025 and resubmitted before this approval.","status":"approved","asOf":"2026-09-22","links":[{"label":"National Natural Science Foundation of China: the world's first integrin-targeted innovative radiopharmaceutical approved, 2 April 2026 (Chinese)","url":"https://www.nsfc.gov.cn/p1/3381/2825/121910.html"},{"label":"Securities Times: approval, phase 3 comparison with FDG PET/CT and the SPECT installed base (Chinese)","url":"https://stcn.com/article/detail/3725436.html"},{"label":"99mTc-3PRGD2 SPECT/CT for diagnosing lymph node metastasis of primary malignant lung tumours (Korean Journal of Radiology, 2023)","url":"https://doi.org/10.3348/kjr.2023.0411"},{"label":"Advances in clinical oncology research on 99mTc-3PRGD2 SPECT imaging (Frontiers in Oncology, 2022)","url":"https://doi.org/10.3389/fonc.2022.898764"}],"tags":["diagnostic","china","spect","integrin"],"related":["integrin-avb3","tc-99m","spect","csnm","china-isotope-radiation","chinese-journal-of-nuclear-medicine-and-molecular-imaging","f-18"],"indications":["nsclc"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Jilunte","code":"99mTc-3PRGD2","modality":"Integrin αvβ3-targeted SPECT imaging agent (RGD peptide dimer)","mechanism":"A technetium-99m-labelled dimeric RGD peptide with three polyethylene glycol spacers that binds integrin αvβ3 on tumour neovasculature and tumour cells, so an ordinary SPECT/CT camera can image the lesion.","approvals":[{"region":"China","year":2026,"indication":"SPECT/CT assessment of regional lymph-node metastasis in patients with suspected lung cancer","note":"NMPA approval 2 April 2026; described by its funder as China's first independently developed Class 1 innovative radiopharmaceutical"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[{"date":"2026-04-02","type":"approval","region":"China","note":"NMPA marketing approval (priority review), trade name Jilunte","source":"https://www.nsfc.gov.cn/p1/3381/2825/121910.html"},{"date":"2025-02","type":"withdrawal","region":"China","note":"An earlier new drug application for the same product was withdrawn before being resubmitted; reported by Chinese trade press, not by the regulator","source":"https://www.163.com/dy/article/K0V13Q6H05118K9D.html"}]},{"id":"tc-99m-maa","kind":"drug","name":"Technetium Tc-99m albumin aggregated (MAA)","aka":["99mTc-MAA","Tc-99m macroaggregated albumin","MAA","Pulmotech MAA","DraxImage MAA"],"tldr":"Tiny clumps of albumin, a normal blood protein, tagged with a radioactive marker and injected into a vein. They wedge briefly in the smallest blood vessels of the lung wherever blood is flowing, so the scan maps the lung's blood supply; the clumps then break up and clear.","summary":"Tc-99m macroaggregated albumin is the perfusion half of the V/Q scan and one of the oldest radiopharmaceuticals still in routine use. Two products are marketed in the US: Pulmotech MAA (BLA 210089, CIS bio International, distributed by Curium, initial US approval 2020) and DraxImage MAA (BLA 017881, Jubilant DraxImage, initial US approval 1987). Both carry the same two indications: lung scintigraphy as an adjunct in the evaluation of pulmonary perfusion in adults and paediatric patients, and peritoneovenous shunt scintigraphy as an aid in evaluating its patency.\n\nDosing is by particle count rather than activity alone. An adult dose is 200,000 to 700,000 particles, about 350,000 recommended, falling to 10,000-50,000 for neonates under four weeks, because each particle occludes a capillary and the margin of safety comes from how few of them there are relative to the pulmonary capillary bed. The labels contraindicate the agent in severe pulmonary hypertension, where deaths have been reported, and in albumin hypersensitivity.\n\nIts second life is in interventional oncology. Before yttrium-90 radioembolisation, MAA is injected into the hepatic artery and imaged to estimate the lung shunt fraction, because hepatopulmonary shunting can deliver enough dose to the lungs to cause radiation pneumonitis. The dose constraint usually applied is a lung mean dose of 30 Gy from a single treatment or 50 Gy cumulative, and a shunt fraction above 20% has traditionally contraindicated resin-microsphere treatment. MAA is used as the surrogate because its particles are close in size to the microspheres, though the correspondence is imperfect and is itself an active research question.","status":"approved","asOf":"2026-09-23","links":[{"label":"FDA label: PULMOTECH MAA (BLA 210089), revised August 2023","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/210089s002lbl.pdf"},{"label":"FDA label: DRAXIMAGE MAA (BLA 017881), revised December 2023","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/017881s030lbl.pdf"},{"label":"Kappadath et al.: lung shunt fraction from 99mTc-MAA SPECT/CT for Y-90 treatment planning, with the 30 Gy single and 50 Gy cumulative lung dose constraints","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC8479035/"}],"tags":["perfusion","V/Q","technetium","radioembolisation work-up"],"related":["technegas","kr-81m","split-function-lung-perfusion","tc-99m","pulmonary-embolism-vq","y-90-resin-microspheres","y-90-glass-microspheres","radioembolisation-tare","curium","jubilant-radiopharma","y-90"],"indications":["pulmonary-embolism-vq"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"Intravenous SPECT particle agent","mechanism":"Human albumin is heat-aggregated into particles of which more than 90% measure 10-90 micrometres, none above 150. Injected intravenously, they are carried to the lungs and physically lodge in pulmonary arterioles and capillaries in proportion to regional blood flow: over 90% are trapped within 1 to 5 minutes, occluding a tiny fraction of the pulmonary capillary bed. The blockade is temporary because the aggregates are fragile and break up, and the resulting image is a perfusion map. Injected instead into the hepatic artery, the same particles follow the route Y-90 microspheres will take, which is what makes them a usable simulation of a radioembolisation treatment.","approvals":[{"region":"US","year":1987,"indication":"Lung scintigraphy as an adjunct in the evaluation of pulmonary perfusion, and peritoneovenous shunt patency","note":"DraxImage MAA, BLA 017881, Jubilant DraxImage"},{"region":"US","year":2020,"indication":"Lung scintigraphy as an adjunct in the evaluation of pulmonary perfusion, and peritoneovenous shunt patency","note":"Pulmotech MAA, BLA 210089, CIS bio International, distributed by Curium"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection for lung perfusion; intra-arterial (hepatic artery) for radioembolisation work-up","schedule":"Adults 200,000-700,000 particles per injection, approximately 350,000 recommended; paediatric doses reduced by age, 10,000-50,000 particles for neonates under four weeks","modifications":"Contraindicated in severe pulmonary hypertension and in albumin hypersensitivity; reduce particle number in right-to-left shunt","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/210089s002lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tc-99m-mdp","kind":"drug","name":"Technetium Tc-99m medronate (MDP)","aka":["99mTc-MDP","Technetium Tc 99m Medronate","CIS-MDP","Draximage MDP-25"],"tldr":"The standard, decades-old bone scan: a radioactive tracer that sticks to areas of bone rebuilding, so a gamma-camera picture afterwards shows where cancer may have spread to bone, or where a fracture or infection is healing.","summary":"Technetium Tc 99m Medronate is supplied as a cold kit -- a vial of medronic acid and stannous chloride that the radiopharmacy reconstitutes with the hospital's own technetium-99m generator eluate -- under several long-approved NDAs (e.g. Draximage MDP-25, NDA 018035; CIS-MDP, NDA 018124). It is indicated broadly as a bone imaging agent to delineate areas of altered osteogenesis, without an oncology-specific label claim, but the single largest clinical use remains detecting osteoblastic skeletal metastases, chiefly from prostate and breast cancer, alongside benign indications such as fracture, infection and metabolic bone disease.\n\nThe recommended adult dose is 370-740 MBq (10-20 mCi) IV, with optimal imaging 1-4 hours later; about half the injected dose is retained in the skeleton and half is excreted in urine within 24 hours. The label carries no listed contraindications but flags allergic dermatological reactions reported with the diphosphonate class, and a 2025 label update added a warning about altered biodistribution in the presence of high levels of certain cations (iron, calcium, aluminium). Despite the rise of 18F-NaF PET and, in prostate cancer, PSMA PET, 99mTc-MDP bone scintigraphy remains the most widely available and lowest-cost skeletal survey worldwide.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Draximage MDP-25 (Kit for the Preparation of Technetium Tc 99m Medronate Injection)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/018035s043lbl.pdf"},{"label":"FDA label: CIS-MDP (Kit for the Preparation of Technetium Tc 99m Medronate)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/018124s013lbl.pdf"}],"tags":["bone scan","SPECT","cold kit","generic"],"related":["f-18-naf","f-18","tc-99m"],"indications":["prostate"],"sections":[],"technologies":["spect","spect-ct","radionuclide-generators-kits"],"targets":[],"drugs":[],"companies":["curium","ge-healthcare"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"SPECT tracer","mechanism":"Medronate (methylene diphosphonate) is a bisphosphonate that chelates technetium-99m and, once injected, adsorbs onto the hydroxyapatite crystal surface of bone in proportion to local osteoblastic activity and blood flow -- the same underlying biology as 18F-NaF PET, but imaged with a conventional gamma camera or SPECT rather than PET.","approvals":[{"region":"US","year":1972,"indication":"Bone imaging agent to delineate areas of altered osteogenesis"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection over ~30 seconds, after kit reconstitution","schedule":"370-740 MBq (10-20 mCi) in an average 70 kg adult; optimal imaging 1-4 hours post-injection","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/018035s043lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tc-99m-psma-imaging","kind":"drug","name":"Technetium Tc-99m PSMA agents (PSMA-I&S)","aka":["99mTc-PSMA-I&S","Tc-99m PSMA imaging and surgery"],"tldr":"A version of the PSMA prostate cancer scan that uses the same cheap, widely available radioactive tag as a standard bone scan instead of the PET tracers. Surgeons can also carry a small radiation detector into the operating room to help find and remove cancerous lymph nodes. It has not been through formal drug approval; it is used as an academic, in-house preparation.","summary":"99mTc-PSMA-I&S ([99mTc]Tc-mas3-y-nal-k(Sub-KuE)) was developed at the Technical University of Munich as a cost-effective, kit-based alternative to 111In-PSMA-I&T for PSMA-targeted radioguided surgery, first reported in the Journal of Nuclear Medicine in 2017. In that first-in-human report, preoperative SPECT/CT at 12 hours after injection showed high uptake in all lesions previously identified by 68Ga-PSMA-11 PET/MR, and a handheld gamma probe successfully guided intraoperative resection of metastatic lymph nodes down to 3 mm.\n\nBeyond radioguided surgery, retrospective single-centre series have used PSMA-I&S SPECT/CT as a stand-alone diagnostic tool: one series reported patient-based sensitivity, specificity and accuracy of 86%, 100% and 92% for detecting primary prostate cancer, and for restaging in biochemical recurrence, sensitivity of 67% with specificity of 100%, generally trailing PSMA-PET's reported sensitivity in the low-PSA setting but offering same-day, low-cost imaging with equipment most nuclear medicine departments already own. Because it is produced from an academic cold-kit under local institutional protocols rather than an FDA- or EMA-reviewed marketing application, it has no formal regulatory approval or labelled dose; reported clinical activities have ranged from roughly 500-700 MBq for combined SPECT-and-surgery protocols.","status":"emerging","asOf":"2026-09-22","links":[{"label":"Robu et al., J Nucl Med 2017: preclinical evaluation and first patient application of 99mTc-PSMA-I&S for SPECT imaging and radioguided surgery in prostate cancer","url":"https://jnm.snmjournals.org/content/58/2/235.full.pdf"},{"label":"Diagnostic value of 99mTc-PSMA-I&S SPECT/CT for prostate cancer detection and staging (2024)","url":"https://pmc.ncbi.nlm.nih.gov/articles/PMC10798073/"}],"tags":["PSMA","SPECT","radioguided surgery","academic cold kit"],"related":["cu-64-sar-bispsma","in-111-pentetreotide","ga-68","tc-99m","in-111"],"indications":["prostate","prostate-bcr"],"sections":[],"technologies":["spect","spect-ct"],"targets":["psma"],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"SPECT tracer","mechanism":"PSMA-I&S (\"imaging and surgery\") is a urea-based small-molecule PSMA inhibitor labelled with technetium-99m via a MAS3 chelator. It binds prostate-specific membrane antigen on prostate cancer cells; because technetium-99m is a gamma emitter available from any hospital's own generator (unlike gallium-68 or fluorine-18, which need a generator or cyclotron dedicated to PET production), it can be used both for pre-operative SPECT/CT localisation and, with a handheld gamma probe, for intraoperative radioguided surgery.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tc-99m-pyrophosphate","kind":"drug","name":"Technetium Tc-99m pyrophosphate","aka":["Tc-99m PYP","PYP"],"tldr":"A bone-scanning radioactive tracer that also sticks to stray protein deposits that build up in a stiffened heart in transthyretin amyloidosis. Comparing how brightly the heart lights up against the ribs on the same scan tells doctors whether this specific, now-treatable type of heart disease is present, usually without needing a heart biopsy.","summary":"Technetium Tc-99m pyrophosphate (Technescan PYP, and generic/branded equivalents such as Phosphotec) is an old bone- and cardiac-imaging kit, FDA-approved for skeletal imaging of altered osteogenesis and, since the 1970s, as an adjunct in diagnosing acute myocardial infarction by direct uptake into necrotic tissue. Its label indications remain that dual scope (plus gated blood pool and gastrointestinal bleeding imaging via in vivo red blood cell labelling); it does not carry an FDA-labelled cardiac amyloidosis indication, and its use for that purpose is guideline-driven, off-label with respect to the original label wording, and now the dominant reason it is ordered in nuclear cardiology.\n\nThe evidence base for amyloid imaging is Gillmore et al. (2016, JAMA Cardiology, n=1,217: 857 with confirmed cardiac amyloidosis, 360 controls), which found 99% sensitivity and 86% specificity for ATTR cardiac amyloidosis using grade 2-3 myocardial uptake on planar/SPECT imaging, rising to 100% specificity and positive predictive value when combined with the absence of a monoclonal light-chain clone on serum/urine testing. ASNC/AHA/ASE/EANM/HFSA/ISA/SCMR/SNMMI multisociety expert consensus recommendations (with a 2021 addendum) formalised the protocol: SPECT or SPECT/CT confirmation of myocardial uptake is required (planar imaging alone is not diagnostic), typically read at both 1 hour and 3 hours after injection, with a visual grade of 2 or 3 classed as strongly suggestive of ATTR-CM, grade 1 as equivocal, and grade 0 as not suggestive.\n\nFDA labelled dosing for cardiac imaging is 370-555 MBq (10-15 mCi) intravenously, with imaging historically recommended 60-90 minutes post-injection for acute infarct detection; amyloid imaging protocols from the nuclear cardiology societies use similar activities with imaging windows out to 3 hours to reduce blood-pool interference.","asOf":"2026-09-22","links":[{"label":"FDA label: Technescan PYP (Tc-99m pyrophosphate), 2025 revision","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/017538s023,018321s026lbl.pdf"},{"label":"Gillmore et al. 2016, JAMA Cardiology: multicentre study of Tc-99m PYP for ATTR cardiac amyloidosis","url":"https://jamanetwork.com/journals/jamacardiology/fullarticle/2546034"},{"label":"ASNC practice points: 99mTc-pyrophosphate imaging for cardiac amyloidosis","url":"https://www.asnc.org/wp-content/uploads/2024/05/ASNC-Practice-Point-99mTechnetium-Pyrophosphate.2016.pdf"}],"tags":["SPECT","cardiac amyloidosis","bone-avid tracer"],"related":["tl-201-chloride","tc-99m-sestamibi","tc-99m"],"indications":["cardiac-amyloidosis-attr"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Technescan PYP","modality":"SPECT tracer","mechanism":"Tc-99m pyrophosphate has a specific affinity for areas of altered osteogenesis (bone turnover) and, at lower concentration, for acutely infarcted myocardium and, incidentally, for transthyretin amyloid deposits in the heart, apparently via co-deposition of calcium/microcalcification within the amyloid fibrils. In cardiac amyloidosis imaging, myocardial retention is graded visually against rib (bone) uptake on a 0-3 scale on SPECT (or SPECT/CT) images obtained roughly 1-3 hours after injection; grade 2 (equal to rib) or grade 3 (greater than rib) uptake is considered positive.","approvals":[{"region":"US","year":1976,"indication":"Skeletal imaging to demonstrate areas of altered osteogenesis"},{"region":"US","year":1976,"indication":"Cardiac imaging as an adjunct in the diagnosis of acute myocardial infarction"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"Cardiac imaging (per FDA label): 370-555 MBq (10-15 mCi); cardiac amyloidosis SPECT protocols (per ASNC/multisociety guidance, off-label with respect to the original infarct indication) use similar activity with imaging at 1 and/or 3 hours","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/017538s023,018321s026lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tc-99m-sestamibi","kind":"drug","name":"Technetium Tc-99m sestamibi","aka":["Sestamibi","MIBI","Miraluma (breast imaging)"],"tldr":"A radioactive tracer injected into a vein that lodges inside heart muscle cells in proportion to blood flow, so a gamma camera picture taken after exercise or a stress drug shows which parts of the heart are not getting enough blood.","summary":"Technetium Tc-99m sestamibi (Cardiolite) is a cationic isonitrile SPECT perfusion agent, FDA-approved in December 1990, supplied as a cold kit reconstituted with generator-eluted Tc-99m and injected intravenously for rest and stress myocardial perfusion imaging. Its first-pass myocardial extraction fraction is 55-68%, lower than thallium-201's 82-88% but adequate because the higher injectable activity and 140 keV photon (near-ideal for gamma cameras) compensate with better image counts and a 6-hour half-life that allows same-day or two-day rest/stress protocols.\n\nThe FDA label indications are detecting coronary artery disease by localising reversible (ischaemic) and non-reversible (infarcted) defects, and evaluating myocardial function to inform patient management. The suggested adult dose range is 370-1,110 MBq (10-30 mCi) per injection; a separate approved indication (as Miraluma) at 740-1,110 MBq is for breast imaging as an adjunct to mammography, outside this cardiac scope.\n\nIn practice sestamibi SPECT (usually gated, giving ejection fraction and wall motion alongside perfusion) is the workhorse test to decide whether a patient with chest pain or an abnormal stress test needs coronary angiography and revascularisation versus medical therapy, and it can also serve as the resting perfusion half of a cardiac sarcoidosis PET/SPECT work-up when PET perfusion tracers are unavailable.","asOf":"2026-09-22","links":[{"label":"FDA label: Cardiolite (technetium Tc-99m sestamibi), revised December 2019","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019785s022lbl.pdf"},{"label":"First-pass myocardial extraction fractions of Tc-99m agents and Tl-201 (J Nucl Med Technol review)","url":"https://tech.snmjournals.org/content/jnmt/35/1/3.full.pdf"},{"label":"ASNC/SNMMI PET nuclear cardiology procedure standard (perfusion tracer comparison and cardiac sarcoidosis protocol)","url":"https://www.asnc.org/wp-content/uploads/2024/06/s12350-016-0522-3.pdf"}],"tags":["SPECT","myocardial perfusion","technetium"],"related":["tc-99m-tetrofosmin","tl-201-chloride","tc-99m","tl-201"],"indications":["coronary-artery-disease","cardiac-sarcoidosis"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Cardiolite","modality":"SPECT tracer","mechanism":"A lipophilic cationic isonitrile complex of Tc-99m that crosses cell membranes passively and accumulates in mitochondria, driven by the mitochondrial and plasma membrane potentials of viable myocytes. Myocardial uptake is proportional to coronary blood flow at the time of injection, with a first-pass extraction fraction of about 55-68% (roughly 65% at rest) that plateaus (\"rolls off\") at high flow rates, so it somewhat underestimates very high flow. Unlike thallium-201 it shows minimal redistribution, so a snapshot taken at stress genuinely reflects flow at the moment of injection, and separate rest and stress doses are needed.","approvals":[{"region":"US","year":1990,"indication":"Detecting coronary artery disease by localising myocardial ischaemia and infarction, and evaluating myocardial function"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"370-1,110 MBq (10-30 mCi) per dose for myocardial imaging (rest and stress doses given separately); imaging typically begins 15-60 minutes after injection","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019785s022lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"technetium-sulfur-colloid","kind":"drug","name":"Technetium Tc-99m sulfur colloid","aka":["Tc-99m sulphur colloid"],"tldr":"Technetium sulfur colloid is the radioactive tracer injected around a breast cancer or melanoma before surgery so the surgeon can find the first lymph node the tumour drains to and remove only that node instead of the whole basin.","summary":"Technetium-99m sulfur colloid has been used for liver, spleen and bone marrow scintigraphy since the 1970s, and the FDA label was extended to lymphatic mapping to localise lymph nodes draining a primary breast tumour or melanoma. Sentinel node biopsy guided by the tracer, often with blue dye, replaced routine axillary dissection in breast cancer and elective node dissection in melanoma after the NSABP B-32 and MSLT-I trials, sparing most patients lymphoedema. Tilmanocept (Lymphoseek), a purpose-designed mannose receptor agent, is the newer alternative.","status":"established","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Technetium_(99mTc)_sulfur_colloid","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Technetium_(99mTc)_sulfur_colloid"},{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=technetium%20tc%2099m%20sulfur%20colloid"}],"tags":["gap-fill","chembl-universe"],"related":["tc-99m"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Technetium Tc 99m Sulfur Colloid Kit","modality":"Radiopharmaceutical for lymphatic mapping and liver, spleen and marrow imaging","mechanism":"Colloidal particles labelled with technetium-99m are taken up by macrophages; injected near a tumour they drain to and lodge in the first (sentinel) lymph nodes, which a gamma probe then finds during surgery.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tc-99m-tetrofosmin","kind":"drug","name":"Technetium Tc-99m tetrofosmin","aka":["Tetrofosmin"],"tldr":"A radioactive tracer, chemically similar to Cardiolite, injected into a vein and taken up by heart muscle in proportion to blood flow; a gamma camera scan after rest and after exercise or a stress drug shows areas with reduced blood supply.","summary":"Technetium Tc-99m tetrofosmin (Myoview), initial US approval 1996, is a diphosphine SPECT perfusion agent supplied as a cold kit for reconstitution with Tc-99m generator eluate. It shares sestamibi's core pharmacokinetic profile: passive, blood-flow-proportional myocardial uptake with negligible redistribution, so separate rest and stress doses are required, and its 140 keV photon suits standard gamma cameras.\n\nThe FDA label covers two indications: myocardial perfusion imaging under rest and/or exercise or pharmacologic stress to delineate regions of reversible ischaemia or infarcted myocardium in patients with known or suspected coronary artery disease, and assessment of left ventricular function (ejection fraction and wall motion) via gated SPECT. The recommended dose range is 185-1,221 MBq (5-33 mCi); on a same-day protocol the first (rest or low-level stress) dose is 185-444 MBq followed 1-4 hours later by 555-1,221 MBq for the second acquisition.\n\nIts first-pass extraction fraction (about 54%) is modestly lower than sestamibi's, and comparative studies (e.g. dipyridamole-stress SPECT in mild-to-moderate CAD) have found sestamibi detects more reversible defects, attributed to tetrofosmin's earlier extraction \"roll-off\" at high flow; both remain widely used interchangeably in routine SPECT MPI.","asOf":"2026-09-22","links":[{"label":"FDA label: Myoview (technetium Tc-99m tetrofosmin), 2022 revision","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/020372Orig1s033lbl.pdf"},{"label":"First-pass extraction fractions of Tl-201, Tc-99m sestamibi and tetrofosmin (Circ Cardiovasc Imaging)","url":"https://www.ahajournals.org/doi/10.1161/circimaging.109.854893"},{"label":"Sestamibi vs tetrofosmin defect detection in mild-to-moderate CAD (JACC 2001)","url":"https://www.jacc.org/doi/10.1016/S0735-1097(00)01148-7"}],"tags":["SPECT","myocardial perfusion","technetium"],"related":["tc-99m-sestamibi","tl-201-chloride","tc-99m"],"indications":["coronary-artery-disease","cardiac-sarcoidosis"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Myoview","modality":"SPECT tracer","mechanism":"A lipophilic cationic diphosphine complex of Tc-99m, taken up by myocytes in proportion to blood flow and retained largely by binding within mitochondria, driven by the transmembrane and mitochondrial potentials, with minimal redistribution after uptake. Its first-pass myocardial extraction fraction is around 54%, similar to but slightly lower than sestamibi's, so its uptake-versus-flow curve plateaus (rolls off) at a somewhat lower flow rate, which can mean smaller apparent defect extent/severity than sestamibi in mild-to-moderate disease.","approvals":[{"region":"US","year":1996,"indication":"Myocardial perfusion imaging under rest and/or exercise or pharmacologic stress to delineate reversible ischaemia and infarcted myocardium"},{"region":"US","year":1999,"indication":"Assessment of left ventricular function (ejection fraction and wall motion)"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"185-1,221 MBq (5-33 mCi) per dose; same-day protocol gives 185-444 MBq first then 555-1,221 MBq 1-4 hours later; imaging can begin 15 minutes after injection","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/020372Orig1s033lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tc-99m-hmpao-brain","kind":"drug","name":"Technetium-99m exametazime (brain perfusion)","aka":["Ceretec","Tc-99m HMPAO","HMPAO"],"tldr":"A cold-kit radioactive tracer that maps blood flow inside the brain on a SPECT scan, used mainly to look for the effects of stroke and, off-label in practice, to help support a diagnosis of brain death.","summary":"Technetium-99m exametazime (Ceretec, GE Healthcare) is a cold kit reconstituted with the user's own technetium-99m generator eluate. Its FDA-labelled indications are cerebral scintigraphy as an adjunct in the detection of altered regional cerebral perfusion in stroke, and, as a separate use of the same kit, radiolabelling of autologous leukocytes for localising intra-abdominal infection and inflammatory bowel disease; it is approved in adults and in paediatric patients aged 2-17. It is a much older, non-specific perfusion agent rather than a targeted molecular tracer: unlike the amyloid, tau and dopamine transporter tracers in this group, HMPAO shows blood flow, not a disease-specific molecular target.\n\nFor cerebral scintigraphy the FDA label recommends 370-740 MBq (10-20 mCi) intravenously, with dynamic imaging in the first 10 minutes and static (planar or SPECT) imaging from 15 minutes up to 6 hours after injection; an SNMMI fact sheet on the brain-death application cites a higher adult range of 370-1110 MBq (10-30 mCi). For leukocyte labelling the recommended adult dose is 185-370 MBq (5-10 mCi) of labelled cells, re-injected within about an hour of labelling. Effective dose at the upper cerebral dose of 1110 MBq is roughly 10.3 mSv.\n\nBeyond its labelled stroke indication, Tc-99m HMPAO brain SPECT is used clinically, per SNMMI practice guidance, as an ancillary test to help confirm the absence of cerebral blood flow in patients with an equivocal clinical diagnosis of brain death, a use it shares conceptually with EEG and cerebral angiography. It has also historically been used for perfusion patterns in dementia work-up, but F-18 FDG PET has largely superseded SPECT perfusion imaging for that purpose because of better spatial resolution and more extensive validation.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA label: Ceretec (technetium Tc99m exametazime kit)","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019829s034lbl.pdf"},{"label":"SNMMI fact sheet: brain death assessment with Ceretec (Tc-99m HMPAO)","url":"https://snmmi.org/common/Uploaded%20files/Web/Education%20and%20Meetings/SNMMI%20Fact%20Sheet_Brain%20Death%20Fact%20Sheet%20Ceretec%20-Tc-99m%20HMPAO.pdf"}],"tags":["SPECT","diagnostic","neurology","perfusion imaging"],"related":["ge-healthcare","spect","f-18-fdg-brain","f-18","tc-99m"],"indications":[],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Ceretec","modality":"SPECT tracer","mechanism":"A lipophilic technetium-99m complex of hexamethylpropyleneamine oxime (HMPAO/exametazime) that crosses the intact blood-brain barrier, is trapped intracellularly by conversion to a hydrophilic species, and distributes in proportion to regional cerebral blood flow, allowing SPECT mapping of brain perfusion.","approvals":[{"region":"US","year":1994,"indication":"Cerebral scintigraphy as an adjunct in the detection of altered regional cerebral perfusion in stroke; and leukocyte-labelled scintigraphy for localising intra-abdominal infection and inflammatory bowel disease"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection (cerebral scintigraphy) or re-injection of labelled autologous leukocytes","schedule":"Cerebral scintigraphy: 370-740 MBq (10-20 mCi) IV; imaging 15 minutes to 6 hours post-injection. Leukocyte labelling: 185-370 MBq (5-10 mCi) of labelled cells, given within about 1 hour of labelling","monitoring":"Visual/semi-quantitative assessment of regional cerebral perfusion on planar or SPECT images","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019829s034lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tilmanocept-tc99m","kind":"drug","name":"Technetium-99m tilmanocept","aka":[],"tldr":"The purpose-built tracer for sentinel lymph node mapping in breast cancer, melanoma and oral cancer, replacing off-label sulfur colloid.","summary":"Technetium-99m tilmanocept is a mannosylated dextran labelled with technetium-99m that binds CD206, the mannose receptor on macrophages in lymph nodes. Because it is small it drains rapidly from the injection site, and because it binds a receptor it stays in the sentinel node rather than passing through to second-echelon nodes, which simplifies surgery. It was the first agent purpose-built for sentinel lymph node mapping, replacing off-label sulfur colloid. The FDA approved it in March 2013 for breast cancer and melanoma, in 2014 for sentinel node localisation in oral cavity squamous cell carcinoma, where mapping showed 97.8% sensitivity, and extended it to children in 2017; the EU approved it in 2014. It is detected with a handheld gamma counter in theatre. Tilmanocept finds the first node a cancer would spread to so that only that node needs removal.","status":"approved","asOf":"2026-09-08","wikipedia":"https://en.wikipedia.org/wiki/Tilmanocept","links":[{"label":"Label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Lymphoseek"}],"tags":["gap-fill","diagnostic"],"related":["tc-99m"],"indications":[],"sections":[],"technologies":["spect"],"targets":[],"drugs":[],"companies":["navidea"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Lymphoseek","modality":"Radiopharmaceutical lymphatic mapping agent","mechanism":"Mannosylated dextran that binds CD206 (mannose receptor) on macrophages in sentinel nodes, giving rapid uptake and low pass-through to second-echelon nodes.","approvals":[{"region":"US","year":2013,"indication":"Lymphatic mapping with a handheld gamma counter in breast cancer and melanoma"},{"region":"US","year":2014,"indication":"Sentinel lymph node localisation in oral cavity squamous cell carcinoma"},{"region":"EU","year":2014,"indication":"Sentinel node imaging in breast cancer, melanoma, oral SCC"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"temozolomide","kind":"drug","name":"Temozolomide","aka":[],"tldr":"The only chemotherapy proven to extend life in glioblastoma, given during and after radiation. It works best when the tumour has switched off a repair gene called MGMT.","summary":"Stupp/EORTC 26981-NCIC (2005): adding concurrent and adjuvant temozolomide to radiotherapy raised median OS from 12.1 to 14.6 months and 2-year survival from 10% to 27%. Benefit concentrates in MGMT-promoter-methylated tumours (median OS ~23 months vs ~13 months unmethylated). Also standard with radiotherapy in grade 3 astrocytoma (CATNON) and, with PCV as an alternative, in oligodendroglioma. Oral, well tolerated; lymphopenia and hypermutation at recurrence are the costs.","status":"standard-of-care","asOf":"2026-09-06","wikipedia":"https://en.wikipedia.org/wiki/Temozolomide","links":[{"label":"Wikipedia","url":"https://en.wikipedia.org/wiki/Temozolomide"}],"tags":[],"related":[],"indications":["glioblastoma"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":["merck"],"institutions":[],"pathways":[],"terms":[],"trials":["nct04919226"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Temodar","modality":"Oral alkylating chemotherapy","mechanism":"Prodrug of MTIC; methylates O6-guanine; cytotoxicity depends on unrepaired lesions when MGMT is silenced.","approvals":[{"region":"US","year":1999,"indication":"Refractory anaplastic astrocytoma"},{"region":"US","year":2005,"indication":"Newly diagnosed glioblastoma with radiotherapy"},{"region":"EU","year":1999,"indication":"Temodal; malignant glioma (recurrent 1999; newly diagnosed glioblastoma with radiotherapy 2005); 26 Jan 1999"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"tl-201-chloride","kind":"drug","name":"Thallous chloride Tl-201","aka":["Thallium-201","Tl-201 chloride"],"tldr":"The original heart-blood-flow tracer: a radioactive form of the metal thallium that heart muscle cells pull in almost like potassium, so a scan straight after exercise and a second scan hours later can tell a starved-but-alive muscle from permanently dead muscle without a second injection.","summary":"Thallous chloride Tl-201 is the oldest of the routine myocardial perfusion agents, taken up by the Na+/K+-ATPase pump with a first-pass extraction fraction of roughly 82-88%, the highest of the perfusion tracers and closest to a linear flow tracer. Its defining clinical property is redistribution: after stress injection, thallium washes out of normally perfused myocardium and re-enters previously ischaemic but viable segments over several hours, so a single injection with stress and delayed (redistribution) imaging can separate ischaemia from infarction/scar and assess viability, a capability the non-redistributing Tc-99m agents lack without a second dose.\n\nThe current FDA label indication is myocardial perfusion imaging (planar or SPECT) for diagnosis of coronary artery disease by localising non-reversible defects (infarction) and reversible defects (ischaemia, with exercise or pharmacologic stress), plus a separate indication for localising parathyroid hyperactivity pre- and post-operatively. Recommended adult doses are 37-74 MBq (1-2 mCi) for planar imaging and 74-111 MBq (2-3 mCi) for SPECT.\n\nBecause thallium's 80 keV and 167 keV photons are lower-energy than technetium's 140 keV, image quality and count statistics are inferior, and the longer 73-hour half-life gives a higher radiation dose per study; the Tc-99m agents and PET tracers have therefore displaced most of thallium's rest/stress workload, but it remains in use, particularly for viability assessment and as the low-dose rest half of dual-isotope protocols.","asOf":"2026-09-22","links":[{"label":"FDA label: Thallous Chloride Tl 201 Injection, 2025 revision","url":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/018150s029lbl.pdf"},{"label":"First-pass extraction fraction comparison table (J Nucl Med Technol review)","url":"https://tech.snmjournals.org/content/jnmt/35/1/3.full.pdf"}],"tags":["SPECT","myocardial perfusion","viability"],"related":["tc-99m-sestamibi","tc-99m-tetrofosmin","tc-99m","tl-201"],"indications":["coronary-artery-disease"],"sections":[],"technologies":[],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"modality":"SPECT tracer","mechanism":"Tl+ is a potassium analogue actively taken up by viable myocytes via the Na+/K+-ATPase pump, giving the highest first-pass myocardial extraction fraction of the routine perfusion agents (about 82-88%) and a near-linear relationship with blood flow across a wide range. Unlike the Tc-99m agents, thallium redistributes over hours as it re-equilibrates between myocardial and blood compartments, which is exploited clinically: a stress image followed by 3-4 hour (or 24 hour) redistribution imaging distinguishes reversible ischaemia (fills in on redistribution) from fixed scar (stays a defect), and can assess myocardial viability without a second injection.","approvals":[{"region":"US","year":1977,"indication":"Myocardial perfusion imaging (planar or SPECT) for diagnosis of coronary artery disease by localisation of infarction and, with stress, ischaemia"},{"region":"US","year":1977,"indication":"Localisation of sites of parathyroid hyperactivity pre- and post-operatively"}],"mechanismSteps":[],"dosing":{"route":"Intravenous injection","schedule":"Planar myocardial imaging 37-74 MBq (1-2 mCi); SPECT myocardial imaging 74-111 MBq (2-3 mCi); parathyroid localisation 75-130 MBq (2-3.5 mCi)","source":"https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/018150s029lbl.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"thyrotropin-alfa","kind":"drug","name":"Thyrotropin alfa","aka":["Recombinant human TSH","rhTSH"],"tldr":"Thyrogen is an injected version of thyroid-stimulating hormone that lets people with thyroid cancer have radioiodine treatment and follow-up blood tests without stopping their thyroid hormone tablets and suffering weeks of hypothyroidism.","summary":"Thyrotropin alfa was approved by the FDA in November 1998 as an adjunctive diagnostic tool for serum thyroglobulin testing with or without radioiodine imaging in the follow-up of well-differentiated thyroid cancer, and in 2007 for pre-therapeutic stimulation before radioiodine remnant ablation after thyroidectomy in patients without distant metastases; the EU authorised Thyrogen in 2000 with the same uses. The HiLo and ESTIMABL trials showed that rhTSH-stimulated low-dose (1.1 GBq) radioiodine ablation is as effective as high-dose ablation after thyroid hormone withdrawal, sparing patients hypothyroid symptoms and reducing radiation exposure. Nausea and headache are the main adverse effects; transient tumour swelling can occur with CNS or spinal metastases. Marketed by Sanofi (Genzyme).","status":"approved","asOf":"2026-09-10","wikipedia":"https://en.wikipedia.org/wiki/Thyrotropin_alfa","links":[{"label":"EPAR (EMA)","url":"https://www.ema.europa.eu/en/medicines/human/EPAR/thyrogen"},{"label":"US label (DailyMed)","url":"https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=thyrotropin%20alfa"}],"tags":["ema-list","supportive"],"related":[],"indications":["thyroid"],"sections":[],"technologies":["radioiodine-therapy"],"targets":[],"drugs":[],"companies":[],"institutions":[],"pathways":[],"terms":["radioiodine-term"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"Thyrogen","modality":"Recombinant human thyroid-stimulating hormone","mechanism":"Recombinant TSH stimulates iodine uptake and thyroglobulin release from thyroid remnants and differentiated thyroid cancer cells, allowing radioiodine ablation and thyroglobulin testing without stopping levothyroxine.","approvals":[{"region":"US","year":1998,"indication":"Adjunctive diagnostic tool for thyroglobulin testing in well-differentiated thyroid cancer; pre-therapeutic stimulation for radioiodine remnant ablation added 2007"},{"region":"EU","year":2000,"indication":"Thyroglobulin testing and radioiodine imaging in thyroid cancer follow-up; pre-therapeutic stimulation for radioiodine ablation"}],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"y-90-glass-microspheres","kind":"drug","name":"Yttrium-90 glass microspheres","aka":["TheraSphere","Y-90 glass microspheres"],"tldr":"Microscopic glass beads containing a radioactive metal are injected into the artery that supplies a liver tumour. The beads stay in place permanently and give off radiation that fades away within about two weeks.","summary":"TheraSphere consists of yttrium-90 fused into glass microspheres and delivered by selective internal radiation therapy (SIRT) through a hepatic artery catheter. It was marketed in the US from 1999-2000 under a Humanitarian Device Exemption (HDE H980006) for unresectable hepatocellular carcinoma (HCC), which limited annual patient numbers.\n\nBoston Scientific (which acquired the product from BTG/Biocompatibles) received full FDA premarket approval (PMA P200029) on 17 March 2021, based on the LEGACY study, a retrospective single-arm, multicentre study of 162 patients with solitary unresectable HCC (1-8 cm). The approved indication is SIRT for local tumour control of solitary tumours 1-8 cm in diameter in patients with Child-Pugh A cirrhosis, no macrovascular invasion and good performance status. LEGACY reported an objective response rate of 72.2% by blinded independent central review and a 76.1% six-month duration-of-response rate.\n\nA post-approval study (multi-compartment dosimetry, MCD-HCC) is ongoing, and a further PMA supplement was cleared by FDA in February 2026. Dosing uses partition-model or MIRD dosimetry to target roughly 100 Gy to the treated liver volume; the microspheres remain permanently implanted.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA: TheraSphere P200029 approval page","url":"https://www.fda.gov/medical-devices/recently-approved-devices/theraspheretm-p200029"},{"label":"FDA: Summary of safety and effectiveness data (P200029)","url":"https://www.accessdata.fda.gov/cdrh_docs/pdf20/P200029B.pdf"},{"label":"Boston Scientific: FDA approval press release, 18 March 2021","url":"https://news.bostonscientific.com/2021-03-18-Boston-Scientific-Receives-FDA-Approval-for-TheraSphere-TM-Y-90-Glass-Microspheres"},{"label":"LEGACY study, Hepatology 2021","url":"https://journals.lww.com/hep/fulltext/2021/11000/yttrium_90_radioembolization_for_the_treatment_of.9.aspx"}],"tags":["radioembolisation","liver","beta emitter"],"related":["y-90-resin-microspheres","ho-166-microspheres","y-90"],"indications":["hcc"],"sections":[],"technologies":["radioembolisation-tare"],"targets":[],"drugs":[],"companies":["boston-scientific"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"TheraSphere","modality":"radioembolisation","mechanism":"Insoluble glass microspheres (15-35 micron diameter) with yttrium-90 built into the glass matrix, infused through a hepatic artery catheter. The spheres remain permanently embedded in the liver and deliver beta radiation locally; about 95% of the yttrium-90 dose is absorbed within roughly 12 days given the isotope's short half-life.","approvals":[{"region":"US","year":2021,"indication":"Selective internal radiation therapy (SIRT) for local tumour control of solitary unresectable HCC (1-8 cm), Child-Pugh A cirrhosis, no macrovascular invasion, good performance status"}],"mechanismSteps":[],"dosing":{"route":"Intra-arterial infusion into the hepatic artery via catheter","schedule":"Single administration per treated liver territory, individualised by partition-model dosimetry aiming for a target absorbed dose","source":"https://www.accessdata.fda.gov/cdrh_docs/pdf20/P200029B.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"y-90-resin-microspheres","kind":"drug","name":"Yttrium-90 resin microspheres","aka":["SIR-Spheres","Y-90 resin microspheres"],"tldr":"Tiny radioactive beads are injected through a small tube into the artery that feeds the liver. They lodge in the tumour and give it radiation from the inside, mostly sparing the rest of the liver.","summary":"SIR-Spheres are yttrium-90-loaded resin microspheres delivered by transarterial radioembolisation (TARE/SIRT). Yttrium-90 is a pure beta emitter with a physical half-life of about 64 hours; delivery via the hepatic artery exploits the fact that liver tumours draw most of their blood supply from that vessel while normal liver parenchyma relies more on the portal vein.\n\nThe device holds the original 2002 FDA premarket approval (PMA P990065) for unresectable metastatic liver tumours from primary colorectal cancer, given together with adjuvant intrahepatic artery chemotherapy (floxuridine, FUDR). In July 2025 the FDA approved a labelling supplement extending the indication to local tumour control of unresectable hepatocellular carcinoma (HCC) in patients with no macrovascular invasion, Child-Pugh A cirrhosis, well-compensated liver function and good performance status, making SIR-Spheres the only US radioembolisation product approved for both indications.\n\nDosing is individualised: activity is planned using body-surface-area or partition (MIRD) dosimetry models with pre-treatment angiography and a technetium-99m macroaggregated albumin scan to check lung shunting before the therapeutic infusion. SIR-Spheres also carry regulatory approval in the EU (2002), Canada (2016), Australia (1998) and other markets.","status":"approved","asOf":"2026-09-22","links":[{"label":"FDA PMA P990065/S014 approval order","url":"https://www.accessdata.fda.gov/scripts/cdrh/cfdocs/cfpma/pma.cfm?ID=P990065S014"},{"label":"FDA: Summary of safety and effectiveness data (HCC supplement)","url":"https://www.accessdata.fda.gov/cdrh_docs/pdf/P990065S014B.pdf"},{"label":"Sirtex: FDA approval for HCC indication (7 July 2025)","url":"https://www.sirtex.com/media/p1kjiw5m/sirtex-medical-announces-fda-approval-hcc-indication-us.pdf"},{"label":"FDA: original SSED for colorectal indication (2002)","url":"https://www.accessdata.fda.gov/cdrh_docs/pdf/p990065b.pdf"}],"tags":["radioembolisation","liver","beta emitter"],"related":["y-90-glass-microspheres","ho-166-microspheres","tc-99m-maa","tc-99m","y-90"],"indications":["hcc"],"sections":[],"technologies":["radioembolisation-tare"],"targets":[],"drugs":[],"companies":["sirtex"],"institutions":[],"pathways":[],"terms":[],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"brand":"SIR-Spheres","modality":"radioembolisation","mechanism":"Biocompatible resin microspheres (20-40 micron diameter) carrying yttrium-90, a pure beta emitter, infused through a catheter into the hepatic artery so they lodge preferentially in the hypervascular tumour bed and irradiate it from within while sparing most healthy liver.","approvals":[{"region":"US","year":2002,"indication":"Unresectable metastatic liver tumours from primary colorectal cancer, with adjuvant intrahepatic artery chemotherapy (FUDR)"},{"region":"US","year":2025,"indication":"Local tumour control of unresectable hepatocellular carcinoma (no macrovascular invasion, Child-Pugh A, well-compensated liver function, good performance status)"}],"mechanismSteps":[],"dosing":{"route":"Intra-arterial infusion into the hepatic artery via catheter","schedule":"Single administration per treated liver territory; activity individualised by body-surface-area or partition-model dosimetry","monitoring":"Pre-treatment angiography and 99mTc-MAA lung-shunt scan; post-treatment imaging for dosimetry","source":"https://www.accessdata.fda.gov/cdrh_docs/pdf/P990065S014B.pdf"},"toxicity":[],"access":[],"regulatoryEvents":[]},{"id":"girentuximab-zr89","kind":"drug","name":"Zirconium-89 girentuximab","aka":["89Zr-DFO-girentuximab","Zircaix"],"tldr":"Zirconium-89 girentuximab is Telix's PET scan that tells whether a kidney mass is clear cell renal cell carcinoma without a biopsy; the phase 3 ZIRCON trial met its endpoints in 2023 and the product is under regulatory review.","summary":"Telix Pharmaceuticals' TLX250-CDx labels the anti-CAIX antibody girentuximab with zirconium-89. In the ZIRCON phase 3 trial of 300 patients with indeterminate renal masses, the scan identified clear cell renal cell carcinoma with high sensitivity and specificity against surgical histology. Telix filed with the FDA, which issued a refusal-to-file letter in 2024 over manufacturing information, and a resubmission followed. A further phase 3 trial is registered.","status":"phase-3","asOf":"2026-09-16","links":[{"label":"ClinicalTrials.gov: trials of Zirconium-89 girentuximab","url":"https://clinicaltrials.gov/search?intr=TLX250-CDx"}],"tags":["pipeline","ctgov-ingest"],"related":["zr-89"],"indications":["rcc"],"sections":[],"technologies":["immuno-pet","pet"],"targets":[],"drugs":[],"companies":["telix"],"institutions":[],"pathways":[],"terms":[],"trials":["nct06750419"],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"provenance":{"editedBy":"Nuclide ingestion (ClinicalTrials.gov v2, curated)","editedOn":"2026-09-16"},"code":"TLX250-CDx","modality":"PET imaging antibody labelled with zirconium-89","mechanism":"Girentuximab binds carbonic anhydrase IX, expressed by nearly all clear cell renal cell carcinomas but not by normal kidney; the zirconium-89 label shows the tumour on PET days after injection.","approvals":[],"mechanismSteps":[],"toxicity":[],"access":[],"regulatoryEvents":[]}]