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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.
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.
A protein on prostate cancer cells that lets doctors both see the cancer on a PET scan and hit it with a radioactive drug.
PSMA is a type II transmembrane glutamate carboxypeptidase; expression increases with grade and castration resistance. Also expressed in tumour neovasculature of other cancers.
15 products aim at PSMA: bispecific antibodies, radioligands, vaccines, 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.
Novartis announced the supplemental filing after the PSMAddition results in 2025. No action date has been disclosed; the year is our estimate. Source
Tumour-associated overexpression or amplification: 1 of 1 label readouts filed under it score protein level or gene copies (PSMA expression by PET (PSMA-positive)), so the medicines rely on the tumour carrying more of it than normal tissue. HPA FOLH1: RNA tissue enhanced (intestine 251 nTPM, prostate 71 nTPM); high antibody staining in 4 normal tissues; highest cancer staining prostate cancer (7 of 7 high). Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Prostate cancer, Renal cell carcinoma); Open Targets associates it with 1 specific cancer type at or above 0.5 (prostate cancer). (Rule 3 of scripts/fetch-target-specificity.ts.)
Sources: PSMA expression by PET (PSMA-positive) label threshold; Human Protein Atlas FOLH1 tissue; Human Protein Atlas FOLH1 pathology; Open Targets ENSG00000086205 associations
First described 1993. Earliest sequence paper UniProt cites for the protein: Israeli R.S. et al, Cancer Res, 1993, "Molecular cloning of a complementary DNA encoding a prostate-specific membrane antigen". Source.
What a pathology or genomic report can say about this target, each with the thresholds approvals use.
Cell lines and mouse models for this target →
PSMA is a type II transmembrane glutamate carboxypeptidase; expression increases with grade and castration resistance. Also expressed in tumour neovasculature of other cancers.
RNA: tissue enhanced (intestine 251 nTPM, prostate 71 nTPM), detected in many normal tissues.
RNA cancer enriched: Prostate Adenocarcinoma 277 pTPM.
Medium only: endometrial cancer.
HPA FOLH1 tissue · HPA FOLH1 pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Prostate cancer | >90% | PSMA PET positivity, metastatic disease | ~10% PSMA-negative or low | PMC |
| Prostate cancer | 80-95% | Cell-surface protein expression, read by PET rather than by sequencing | Immunohistochemistry across a panel of normal and malignant tissues found PSMA in 33 of 35 primary prostate adenocarcinomas, 7 of 8 lymph node metastases and 8 of 18 bone metastases, with detectable expression among normal tissues confined to prostatic epithelium, duodenal mucosa, a subset of proximal renal tubules and a subpopulation of neuroendocrine cells in colonic crypts; all other normal tissues, including cerebral cortex and cerebellum, were undetectable (Silver 1997). In practice the PET equivalent of that figure is the screening yield: 200 of 291 men screened for TheraP were eligible on imaging, 69%, with PSMA-low disease or FDG-positive PSMA-negative sites the reason for exclusion (Hofman 2021). | 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.
Florastamin is FutureChem's fluorine-18 PSMA PET tracer from South Korea, in phase 3 trials for staging high-risk and recurrent prostate cancer alongside the established PSMA agents.
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.
INO-5401 is an experimental cancer vaccine from Inovio Pharmaceuticals in phase 2 trials for glioma & glioblastoma, aimed at PSMA.
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 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.
This is the paper Europe PMC returns for registry id NCT03392428 with the most citations, so it is the natural first reading for anyone following the TheraP trial. Read the abstract above alongside the trial page and the registry entry; the record was linked automatically and its figures have not been checked by hand.
This academic programme is what the FDA approved 68Ga-PSMA-11 on in December 2020, and the Illuccix and Locametz kits rest on it for the staging indication. Its message for a man being staged before surgery is that a positive PSMA PET node is very likely real, but a negative scan does not rule out small nodal deposits, so the lymph node dissection still matters.
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).
PSMA PET-CT is the preferred staging investigation for high-risk prostate cancer and for biochemical recurrence, though most treatment trials were designed with conventional imaging.
It is the evidence behind using PSMA PET when PSA rises after treatment, and it quantifies the limit that matters most: below PSA 0.5 ng/mL, where salvage radiotherapy works best, the scan is negative in nearly two men in three, so a negative scan is not a reason to wait.
It is the anatomical basis for PSMA imaging and PSMA radioligand therapy, and it predicted two of the practical problems three decades early: salivary, lacrimal and renal uptake as sources of toxicity, and falling expression in dedifferentiated disease as the reason some men are ineligible for treatment.
Query 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.
Shares Uwe Haberkorn, Ken Herrmann, University Hospital Düsseldorf / CIO Düsseldorf, Heidelberg University Hospital / NCT / DKFZ and the tags theranostic, pet-target.
Shares POINT Biopharma, Auger-electron therapy, Perspective Therapeutics, Radioligand plus DNA-repair inhibitor combinations and the tag theranostic.
Shares Radioligand therapy (beta emitters), Prostate cancer and the tag theranostic.
Shares Antigen and the tag pet-target.
Shares Clemens Kratochwil, Uwe Haberkorn, Ken Herrmann, Heidelberg University Hospital / NCT / DKFZ.
Shares Shahneen Sandhu, Declan G. Murphy, Michael Hofman, Theranostics.
Shares Michael J. Morris, A. Oliver Sartor, VISION, VISION: lutetium-177 PSMA-617 radioligand therapy extends survival in advanced prostate cancer.
Shares Piflufolastat F-18 / Pylarify TruVu, Actinium-225 PSMA agents, Radio-antibody & radio-ADC, VISION.