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actinium (225Ac) vipivotide tetraxetan (AAA817, [225Ac]Ac-PSMA-617) is an investigational targeted alpha-particle radioligand therapy developed by Novartis (via its subsidiary Advanced Accelerator Applications) for the treatment of prostate-specific membrane antigen (PSMA)-positive prostate cancer, including metastatic castration-resistant prostate cancer (mCRPC). The drug consists of the PSMA-targeting ligand vipivotide tetraxetan (PSMA-617) conjugated to the alpha-emitting radioisotope actinium-225. It binds specifically to PSMA on the surface of prostate cancer cells, where it is internalized and delivers high-energy alpha radiation over a very short range, causing lethal double-strand DNA breaks in the tumor cells while sparing surrounding healthy tissue. It is currently being evaluated in Phase III clinical trials.
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