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PSMA-directed radioligands are a class of targeted radiopharmaceuticals designed to bind to prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase 2, which is highly overexpressed on the surface of prostate cancer cells. These agents typically consist of a PSMA-targeting ligand (such as a small molecule, peptide, or antibody) conjugated via a linker to a radioactive isotope. Depending on the isotope used, they can serve diagnostic purposes (e.g., gallium-68 or fluorine-18 for PET imaging) or therapeutic purposes (e.g., beta-emitters like lutetium-177 or alpha-emitters like actinium-225 to deliver localized cytotoxic radiation). This theranostic approach allows for precise patient selection, treatment planning, and targeted destruction of PSMA-expressing tumor cells while sparing surrounding healthy tissues.
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