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**Actinium-225 vipivotide tetraxetan** is an investigational, targeted radiopharmaceutical therapy for metastatic castration-resistant prostate cancer (mCRPC). It consists of vipivotide tetraxetan, a small-molecule ligand (based on PSMA-I&T or PSMA-617), which binds specifically to prostate-specific membrane antigen (PSMA) highly expressed in prostate cancer cells. It is radiolabeled with actinium-225, an alpha-emitting radioisotope, allowing the molecule to deliver highly potent, short-range alpha-particle radiation directly to PSMA-expressing tumor cells. This minimizes damage to adjacent healthy tissues and allows for highly targeted cytotoxicity. The approach represents an advance over beta-emitting therapies like lutetium-177 vipivotide tetraxetan. Actinium-225 vipivotide tetraxetan is currently evaluated in clinical trials, notably in the TATCIST trial in patients with mCRPC, including those previously treated with beta-emitting PSMA radioligands.
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