Actinium-225 PSMA-617 — Investigational Agent
Radiopharmaceutical · Phase 1/2 · Novartis
Mechanism of Action
225Ac-PSMA-617 is an alpha-emitting radiopharmaceutical. It consists of the PSMA-617 ligand, which targets the Prostate-Specific Membrane Antigen (PSMA), chelated to the alpha-emitter Actinium-225. Upon binding to PSMA-expressing prostate cancer cells, the complex is internalized. The alpha particles emitted by 225Ac have high linear energy transfer (LET) and a short range (50-100 micrometers), causing dense double-strand DNA breaks that are difficult for the cell to repair, leading to cell death even in resistant tumors.
Investigational Indications
- Metastatic castration-resistant prostate cancer (mCRPC)
- mCRPC progressed after 177Lu-PSMA-617