PSMA
A protein on prostate cancer cells that lets doctors both see the cancer on a PET scan and hit it with a radioactive drug.
Overview
Prostate-specific membrane antigen is the archetypal theranostic target. PSMA PET (Pylarify, Illuccix, Locametz, Pylarify TruVu) is standard for staging; 177Lu-PSMA-617 (Pluvicto) is approved before and after chemotherapy in metastatic castration-resistant prostate cancer. Alpha-emitting 225Ac-PSMA agents and PSMA-targeted bispecifics and CAR-T are in trials.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · A protein on prostate cancer cells that lets doctors both see the cancer on a PET scan and hit it with a radioactive drug.
Backbone ribbon from PDB 3D7H. RCSB PDB 3D7H. The ribbon widens where the chain is folded into a regular pattern and narrows where it is a loose loop.
Same urea-based binding motif as the PSMA-617 and PSMA-11 ligands; not those molecules themselves.
- 1 · What it is
A protein on prostate cancer cells that lets doctors both see the cancer on a PET scan and hit it with a radioactive drug.
- 2 · What goes wrong in cancer
PSMA is a type II transmembrane glutamate carboxypeptidase; expression increases with grade and castration resistance. Also expressed in tumour neovasculature of other cancers.
- 3 · How drugs use it
18 products aim at PSMA: bispecific antibodies, radioligands, imaging agents and other agents. Because it sits on the outside of the cell, it can be reached from the bloodstream: antibodies flag the cell, ADCs deliver a toxin, radioligands deliver radiation, and CAR-T or bispecifics bring a T cell.
External identifiers
Companion diagnostics
- PSMA PET (Ga-68 PSMA-11, F-18 piflufolastat, F-18 flotufolastat) · At least one PSMA-positive lesion and no dominant PSMA-negative lesion (VISION criteria) for lutetium-177 PSMA-617
Biology
PSMA is a type II transmembrane glutamate carboxypeptidase; expression increases with grade and castration resistance. Also expressed in tumour neovasculature of other cancers.
- Prostate cancer (>90%)
- Neovasculature of RCC, glioma, others
How often this target appears
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Prostate cancer | >90% | PSMA PET positivity, metastatic disease | ~10% PSMA-negative or low | PMC |
| Renal cell carcinoma | 60-80% | Neovascular PSMA expression | Clear-cell; imaging studies | PMC |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
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.
AAA817 is an experimental radioligand therapy from Novartis Pharmaceuticals in phase 3 trials for prostate cancer, aimed at PSMA.
Alpha-emitting PSMA drugs that produce responses even after Pluvicto fails, held back mainly by isotope supply.
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.
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.
Flotufolastat is a third PSMA PET tracer, with a radiohybrid chemistry designed to be reused for therapy.
FPI-2265 is an experimental radioligand therapy from Fusion Pharmaceuticals in phase 2 trials for prostate cancer, aimed at PSMA.
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.
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.
Telix's ready-to-label kit that lets any nuclear medicine department make the gallium PSMA scan for prostate cancer.
JNJ-87189401 is an experimental costimulatory agent from Janssen Research & Development in phase 3 trials for prostate cancer, aimed at PSMA.
Novartis' gallium PSMA scan kit, approved the same day as Pluvicto as the test that qualifies men for that radioactive drug.
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.
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.
A radioactive drug that seeks out PSMA on prostate cancer cells; the best-selling radiopharmaceutical ever.
Piflufolastat F-18 (Pylarify) is the leading PSMA PET tracer for prostate cancer, with a new formulation approved in March 2026.
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.
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.
An alpha-emitting radioactive drug built on a PSMA-targeting antibody, rather than the small-molecule ligands used in existing PSMA therapies, was safe enough to move into further testing and shrank PSA in roughly a third to a half of heavily pre-treated men, including some whose cancer had already stopped responding to lutetium-177 PSMA therapy.
Men with metastatic castration-resistant prostate cancer that has progressed after hormonal therapy and chemotherapy, and whose tumours show PSMA on a PET scan, can now receive lutetium-PSMA, which extends life, controls pain and is usually better tolerated than further chemotherapy. It has established a new treatment class in which a scan decides who gets the matching radioactive drug, and it is now being tested earlier in the disease (PSMAfore, PSMAddition).
This was the first evidence, in two patients, that attaching a more powerful (alpha-emitting) form of radiation to the same PSMA-seeking molecule used in lutetium-177 PSMA therapy could produce a complete response even in prostate cancer that had already stopped responding to the beta-emitter version.
Latest papers
topQuery for this target: (TITLE:"PSMA" OR ABSTRACT:"PSMA" OR TITLE:"FOLH1" OR ABSTRACT:"FOLH1") AND (radiopharmaceutical OR radioligand OR radionuclide OR theranostic OR "nuclear medicine" OR "molecular imaging" OR radiotracer OR scintigraphy OR cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about PSMA, not a curated reading list.
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