actinium-225 PSMA-R2

Actinium-225 PSMA-R2 is a targeted alpha-therapeutic (TAT) radiopharmaceutical being developed by Novartis. It consists of the alpha-emitting radioisotope actinium-225 conjugated to PSMA-R2, a next-generation ligand designed to target the prostate-specific membrane antigen (PSMA), which is highly expressed on the surface of prostate cancer cells. Upon binding to PSMA, the compound is internalized, and the actinium-225 delivers high-energy alpha particles directly to the tumor cells. These alpha particles have a short range (micrometers) but high linear energy transfer (LET), causing lethal double-strand DNA breaks while minimizing damage to surrounding healthy tissue. The drug is currently being evaluated in the Phase 1/2 SatisfACtion trial for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC) and metastatic castration-resistant prostate cancer (mCRPC), including patients who have previously received lutetium-177 PSMA radioligand therapy.

Other names

225Ac-PSMA-R2[225Ac]Ac-PSMA-R2actinium (225Ac) PSMA-R2