Radioligand therapy (beta emitters)
A drug that finds tumour cells and carries a radioactive atom that irradiates them from inside the body.
Overview
177Lu-DOTATATE (Lutathera, 2018) in neuroendocrine tumours and 177Lu-PSMA-617 (Pluvicto, 2022; pre-chemotherapy label 2025; 2026 label expansion) in prostate cancer are the approved beta-emitter therapies. Pipeline: 177Lu-FAP, 177Lu-PSMA-I&T, 177Lu-NeoB (GRPR), 177Lu-labelled antibodies. Dosimetry-guided personalised dosing is emerging.
- PSMA / SSTR-positive cell
How it works
177Lu emits beta particles with ~2 mm range and gamma photons for SPECT imaging; the ligand determines biodistribution.
- Systemic, whole-body targeting of microscopic disease
- Crossfire kills antigen-negative neighbours
- Imaging companion selects patients
- Marrow and kidney dose
- Isotope logistics (6.7-day half-life)
- Not curative alone
Dependencies
Open the dependency map →Dependencies are what this technology cannot be delivered without: manufacturing steps, instruments, software, upstream methods. See its full chain on the map.
High-dose radioactive MIBG delivers radiation from inside neuroblastoma cells that take up noradrenaline; used for relapsed disease and tested in upfront therapy.
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.
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.
A FAP-targeted theranostic pair: one version images almost any solid tumour, the other treats it with radiation.
The PET scan for neuroendocrine tumours that finds far more disease than older scans and confirms eligibility for lutetium radioligand therapy (the theranostic pair).
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.
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.
Novartis' gallium PSMA scan kit, approved the same day as Pluvicto as the test that qualifies men for that radioactive drug.
Lutetium-177 dotatate was the first modern radioligand therapy (2018), for neuroendocrine tumours, and is now used in first line.
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.
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 radioactive drug that seeks out PSMA on prostate cancer cells; the best-selling radiopharmaceutical ever.
The original targeted radiotherapy: thyroid cells soak up iodine, so radioactive iodine destroys leftover thyroid tissue and metastases while sparing everything else.
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.
Patients newly diagnosed with an advanced grade 2 or 3 neuroendocrine tumour of the gut or pancreas that shows somatostatin receptors on imaging can now receive lutetium dotatate as their first treatment, gaining more than a year of additional disease control and a much higher chance of tumour shrinkage. It does not settle whether radioligand therapy is better than other first-line options such as capecitabine-temozolomide or everolimus, and long-term marrow safety with earlier use needs surveillance.
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 paper is a map of the radioactive-cancer-drug field at a pivotal moment, explaining to non-specialists and drug developers alike why these treatments work differently from chemotherapy and what needed to be fixed - supply, dosing science, regulation - before more of them could reach patients.
Latest papers
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