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.
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.
- 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
6 products aim at PSMA: radioligands and imaging 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.
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 common it is, by cancer
| 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.
Alpha-emitting PSMA drugs that produce responses even after Pluvicto fails, held back mainly by isotope supply.
Flotufolastat is a third PSMA PET tracer, with a radiohybrid chemistry designed to be reused for therapy.
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.
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.
Latest papers
topQuery for this target: (TITLE:"PSMA" OR ABSTRACT:"PSMA" OR TITLE:"FOLH1" OR ABSTRACT:"FOLH1") AND (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.
Pages like this
not linked directly; found by shared links- TargetFAP
Shares Uwe Haberkorn, University Hospital Düsseldorf / CIO Düsseldorf, Heidelberg University Hospital / NCT / DKFZ, Targeted alpha therapy and the tags theranostic, pet-target.
- TargetSomatostatin receptor 2
Shares Perspective Therapeutics, Auger-electron therapy, Radioligand plus DNA-repair inhibitor combinations, IRCCS Istituto Romagnolo per lo Studio dei Tumori 'Dino Amadori' (IRST) and the tag theranostic.
- TargetGRPR (gastrin-releasing peptide receptor)
Shares Radioligand therapy (beta emitters), Prostate cancer and the tag theranostic.
- TargetTROP2
Shares Antigen and the tag pet-target.
- TermTheranostics
Shares Clarity Pharmaceuticals, PSMA PET → PSMA radioligand therapy, IRCCS Istituto Romagnolo per lo Studio dei Tumori 'Dino Amadori' (IRST), Inselspital, Bern University Hospital / University Cancer Center Inselspital.
- RoadmapRadiopharmaceutical roadmap: iodine → lutetium → actinium
Shares Piflufolastat F-18 / Pylarify TruVu, VISION, Actinium-225 PSMA agents, Radio-antibody & radio-ADC.
- InstitutionEuropean Association of Nuclear Medicine
Shares Clemens Kratochwil, Uwe Haberkorn, Heidelberg University Hospital / NCT / DKFZ, Lutetium-177 vipivotide tetraxetan.
- IdeaA university cyclotron network with shared regulatory files for new tracers
Shares Michael Hofman, Uwe Haberkorn, Heidelberg University Hospital / NCT / DKFZ, Targeted alpha therapy.