PSMA

Ongoing clinical trials and approved products targeting PSMA, in radioligand therapy and PET/SPECT imaging. Data as of 26 October 2026.

Theranostic pair: this target is explored in both imaging and therapy.

Target note

Full name

Prostate-specific membrane antigen (glutamate carboxypeptidase II, FOLH1 gene)

Nature

Type II transmembrane glycoprotein with enzymatic activity (folate hydrolase, NAAG peptidase), internalized after ligand binding.

Normal expression

Prostate epithelium, salivary and lacrimal glands, proximal renal tubules, small intestine, central nervous system.

Disease expression

Overexpressed in the vast majority of prostate adenocarcinomas, all the more so with higher grade and castration-resistant disease. Also expressed by the neovasculature of many solid tumors (kidney, glioma, hepatocellular carcinoma, salivary gland tumors).

Value

The most validated target in radioligand therapy: high tumor expression, internalization, patient selection by PSMA PET, small ligands that are easy to label.

Approaches

Urea-based small molecules (PSMA-617, PSMA-I&T, rhPSMA, albumin binders), antibodies (J591/rosopatamab), β⁻ emitters (¹⁷⁷Lu, ¹⁶¹Tb) and α emitters (²²⁵Ac, ²¹²Pb, ²¹¹At).

Indications explored

Castration-resistant prostate cancer (VISION, PSMAfore), hormone-sensitive (PSMAddition), oligometastatic and neoadjuvant settings; exploratory work in kidney cancer, salivary gland tumors and gliomas.

Points of caution

Xerostomia (marked with ²²⁵Ac), renal and bone marrow toxicity. Heterogeneous tumors, tumors discordant on FDG PET or with neuroendocrine differentiation lose PSMA expression.

Approved products

Ongoing therapy trials · 138Open in the radar →

Ongoing imaging trials · 108Open in the radar →

Cite this page

PSMA. Theranostic Atlas, LaRadiopharmacie.fr. Data as of 26 October 2026. https://theranosticatlas.com/target/psma/ (accessed [date]).

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