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225Ac-rhPSMA-10.1 is an investigational radiohybrid (rh) Prostate-Specific Membrane Antigen (PSMA)-targeted therapeutic radiopharmaceutical designed for the treatment of prostate cancer, specifically metastatic castration-resistant prostate cancer (mCRPC). It is a next-generation alpha-emitting radioligand therapy that selectively binds to PSMA, a protein highly expressed on prostate cancer cells, delivering targeted alpha radiation via actinium-225 to induce tumor cell death while sparing surrounding healthy tissue. Preclinical studies have demonstrated high PSMA binding affinity, efficient cellular internalization, and significant tumor growth suppression in prostate cancer models at much lower radioactivity compared to beta-emitting analogs such as 177Lu-rhPSMA-10.1[4][5][6]. The drug is being developed by Blue Earth Therapeutics and has entered phase 1/2 clinical trials for mCRPC[2].
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