Drug intelligence / Profile preview

Ac-225-PSMA-62

Development stage
Phase 1
Lead developer
POINT Biopharma
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

[Ac-225]-PSMA-62 is a next-generation prostate-specific membrane antigen (PSMA)-targeting radioligand therapy. It consists of the alpha-emitting radioisotope actinium-225 (Ac‑225), a chelating moiety, an optimized linker, and PSMA‑62—a small peptide inhibitor of PSMA. This design enables high-affinity binding to PSMA on prostate cancer cells and promotes efficient internalization into tumor cells. The improved linker technology enhances cellular uptake and tumor retention while facilitating rapid renal clearance to reduce off-target toxicity. [Ac‑225]‑PSMA‑62 is being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC) and oligometastatic hormone-sensitive prostate cancer (OmHSPC). It is currently under investigation in phase Ia/Ib/II clinical trials to assess safety, tolerability, optimal dosing schedules, and efficacy compared with standard-of-care therapies[1][2][3][5].

Other names
Ac-225 PSMA 62Ac225 PSMA 62Ac 225 PSMA 62
02

Targets

PSMA (Prostate-specific membrane antigen)

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