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211At-NpG-PSMA is an alpha-emitting radioligand therapy (RLT) designed to target prostate-specific membrane antigen (PSMA), which is highly expressed in prostate cancer cells. The compound consists of the alpha-particle emitting radioisotope Astatine-211 ($^{211}$At) conjugated to a small-molecule PSMA ligand (NpG-PSMA). Unlike beta-emitting radiopharmaceuticals such as Lutetium-177, alpha particles possess high linear energy transfer (LET) and a very short range in tissue (50–100 μm), allowing for the delivery of potent, localized radiation that induces complex double-strand DNA breaks while sparing adjacent healthy tissue. This agent is primarily being investigated for the treatment of metastatic castration-resistant prostate cancer (mCRPC) in patients who have exhausted standard-of-care options, including androgen receptor signaling inhibitors and taxane-based chemotherapy.
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