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Actinium-225-macropa-pelgifatamab (BAY3546828) is a targeted alpha therapy (TAT) being developed by Bayer for the treatment of metastatic castration-resistant prostate cancer (mCRPC). The drug is a radiopharmaceutical conjugate consisting of a monoclonal antibody, pelgifatamab, which specifically targets the prostate-specific membrane antigen (PSMA) expressed on the surface of prostate cancer cells. This antibody is linked via a macropa chelator to the alpha-emitting radioisotope actinium-225. Upon binding to PSMA-positive cells, the actinium-225 delivers high-energy, short-range alpha radiation, causing lethal double-strand DNA breaks in the target cancer cells while minimizing damage to surrounding healthy tissue. It is currently being evaluated in Phase 1 clinical trials for patients with advanced mCRPC who have limited treatment options.
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