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177Lu-PSMA-597 is a therapeutic radiopharmaceutical consisting of the beta-emitting radioisotope lutetium-177 conjugated to the novel PSMA-targeting peptide PSMA-597. It is designed to treat metastatic castration-resistant prostate cancer (mCRPC) by binding to prostate-specific membrane antigen (PSMA) expressed on the surface of prostate cancer cells. Once bound, the agent is internalized, and the lutetium-177 delivers targeted ionizing radiation, causing DNA damage and cell death in the tumor cells while sparing surrounding healthy tissue. It is currently being evaluated in the Phase II OPTIMAL-PSMA trial to optimize dosing regimens and receptor intensification.
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