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.