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Actinium-225 PSMA (225Ac-PSMA) is a targeted alpha therapy (TAT) radiopharmaceutical platform designed for the treatment of prostate cancer, particularly metastatic castration-resistant prostate cancer (mCRPC). It consists of a prostate-specific membrane antigen (PSMA)-targeting ligand (such as PSMA-617 or PSMA-I&T) conjugated to the alpha-emitting radioisotope actinium-225 (225Ac). Upon administration, the radioligand binds specifically to PSMA-expressing prostate cancer cells, where the actinium-225 decays, emitting high-energy alpha particles over a short range. This localized radiation induces double-stranded DNA breaks, leading to tumor cell death while minimizing damage to surrounding healthy tissues.
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