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225Ac-PSMA-R2

Development stage
Phase 2
Lead developer
Novartis
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
Administration
Intravenous
01

Overview

225Ac-PSMA-R2 is an investigational radiopharmaceutical drug developed for the treatment of prostate cancer, specifically targeting metastatic hormone-sensitive prostate cancer (mHSPC) and metastatic castration-resistant prostate cancer (mCRPC). The drug consists of a ligand, PSMA-R2, which binds to the prostate-specific membrane antigen (PSMA) highly expressed on prostate cancer cells. This ligand is conjugated to actinium-225 (225Ac), a radioactive isotope that emits alpha particles. Upon binding to PSMA-expressing tumor cells, the alpha radiation from actinium-225 induces targeted cytotoxicity by causing double-stranded DNA breaks in the cancer cells while minimizing damage to surrounding healthy tissue. The mechanism of action is thus based on targeted delivery of ionizing radiation directly to tumor sites. Clinical trials are ongoing in Phase I/II stages to evaluate safety, tolerability, and anti-tumor activity in patients who have previously received other anti-cancer treatments[1][2][4][5].

Other names
225 Ac PSMA R2
02

Targets

PSMA (Prostate-specific membrane antigen)

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