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212Pb-PSMA is a targeted alpha therapy (TAT) radiopharmaceutical developed by Orano Med for the treatment of prostate cancer. It comprises a peptide ligand designed to bind with high affinity to the prostate-specific membrane antigen (PSMA), a protein significantly overexpressed on the surface of prostate cancer cells. The peptide is conjugated to lead-212 (212Pb), a radioisotope that acts as an in vivo generator of alpha particles. Upon binding to PSMA and subsequent internalization into the cancer cell, the decay of 212Pb releases high-energy alpha radiation. This radiation causes complex, difficult-to-repair double-strand DNA breaks, leading to cell death. This targeted approach is intended to maximize therapeutic efficacy against tumor cells while minimizing exposure and damage to surrounding healthy tissues.
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