Prostate-specific membrane antigen (PSMA), encoded by the FOLH1 gene, is a transmembrane glycoprotein overexpressed roughly 100- to 1,000-fold in prostate cancer cells compared with most normal tissues. The expression is largely independent of disease stage and androgen-receptor signaling, which makes PSMA one of the cleanest targets in oncology drug development.
The target's clinical breakthrough came through peptide-guided radioligand therapy. Novartis's Pluvicto (lutetium-177 PSMA-617) uses a small-molecule peptide ligand bound to a lutetium-177 radioisotope to deliver targeted internal radiation to PSMA-positive cells. The Phase 3 VISION trial supported the FDA approval in March 2022 for metastatic castration-resistant prostate cancer (mCRPC) after androgen-receptor inhibition and taxane chemotherapy; Pluvicto generated more than $1 billion in 2024 sales. PSMA-PET imaging agents (Pylarify, Locametz, Posluma) became standard of care for prostate-cancer staging shortly afterward.
The next generation of PSMA programs combines the target with a second cancer marker. MultiValent Biotherapies, which launched on June 16, 2026 with a $27M Series A, is developing MVB-101, a PSMA × folate-receptor-alpha (FRα) dual-target peptide-drug conjugate licensed from Coherent Biopharma. Phase 1b/2a is expected to start Q3 2026. Other sponsors are advancing PSMA-targeted small-molecule conjugates and bispecific T-cell engagers.
Stories here cover PSMA-targeted drug development and the radioligand-and-PDC competitive set. See [[prostate-cancer]], [[peptide-drug-conjugate]], and [[mvb-101]] for adjacent threads.
MultiValent Biotherapies announced June 16 a first closing of $27.425 million in Series A financing to advance MVB-101, a PSMA × folate-receptor-alpha (FRα) dual-target peptide-drug conjugate licensed from China-based Coherent Biopharma (originally CBP-1018). MVB-101 binds two validated prostate-cancer targets simultaneously; existing PDCs and radioligand therapies (Pluvicto, Lutathera) hit one target each. MultiValent holds exclusive global rights outside greater China. A Phase 1b/2a clinical trial in a subgroup of prostate cancer patients is planned to start in Q3 2026. The launch adds another oncology PDC to a field still dominated by Pluvicto (lutetium-177 PSMA-617), Lutathera, and Pfizer's AVA6000 FAP-Dox.
Telix Pharmaceuticals reported ProstACT Global Phase 3 Part 1 data at ASCO 2026 as a late-breaking presentation. TLX591-Tx (lutetium-177 rosopatamab tetraxetan) — a PSMA-targeted lutetium radio-antibody-drug conjugate — met its primary safety objectives in the safety and dosimetry lead-in, demonstrating an acceptable tolerability profile with no new safety signals when combined with enzalutamide (Xtandi), abiraterone (Zytiga), or followed by docetaxel in PSMA-positive metastatic castration-resistant prostate cancer (mCRPC). ProstACT Global is an international Phase 3 trial evaluating TLX591-Tx plus standard of care versus standard of care alone. The drug sits in the PSMA-targeted radioligand class alongside Novartis's approved Pluvicto (lutetium-177 PSMA-617, a peptide-based radioligand), but uses an antibody rather than a small-molecule peptide as the targeting vector. The PSMA radioligand field — Pluvicto, ProstACT, plus the Aktis AKY-2519 B7-H3 miniprotein radioconjugate covered earlier this week — is one of the fastest-growing targeted-conjugate categories in oncology.
The ASCO 2026 Annual Meeting opened today at McCormick Place Chicago, running through June 2, with more than 7,000 abstracts. The peptide-and-targeted-conjugate oncology cohort — pre-released in the May 21 abstract drop and the May 26 embargoed press briefing — now moves to live presentation. Friday May 29 brought the Corbus CRB-701 Nectin-4 ADC cervical/OPSCC data and the Dana-Farber/Bristol multiple myeloma and Pfizer lung cancer readouts. The peptide-mechanism slate across the meeting: Bicycle Therapeutics zelenectide pevedotin Duravelo-2 (bicyclic peptide-MMAE conjugate, oral June 1); Avacta AVA6000 FAP-Dox; BriaCell Bria-IMT cell-and-peptide immunotherapy; Sapience lucicebtide C/EBPβ antagonist (GBM); Aktis AKY-2519 B7-H3 miniprotein radioconjugate; Mayo TPIV200 folate-receptor peptide vaccine (TNBC, June 1); Telix ProstACT PSMA radioligand (June 1); plus the GLP-1 cancer slate (Abstract 3143, Roswell Park breast cancer). The targeted-conjugate categories — Nectin-4, PSMA, B7-H3, FAP, SSTR2 — are the densest peptide-adjacent oncology competition at the meeting.