PSMA-targeting radiopharmaceuticals

PSMA-targeting radiopharmaceuticals are a class of targeted imaging and therapeutic agents designed to bind to prostate-specific membrane antigen (PSMA), a cell-surface protein highly overexpressed in prostate cancer cells and tumor neovasculature. These agents consist of a PSMA-targeting moiety—ranging from low-molecular-weight urea-based ligands (such as PSMA-617 and PSMA-11) to monoclonal antibodies (such as J591)—conjugated via a linker and chelator to a radionuclide. For diagnostic applications (theranostics), positron-emitting or single-photon-emitting isotopes (e.g., gallium-68, fluorine-18) are utilized for PET/SPECT imaging to localize metastatic lesions. For therapeutic applications, beta-emitting (e.g., lutetium-177) or alpha-emitting (e.g., actinium-225) radionuclides are employed to deliver localized, cytotoxic radiation directly to the cancer cells, minimizing damage to surrounding healthy tissues.

Other names

PSMA-targeted radioligand therapyPSMA-targeted radionuclide therapyPSMA-targeted radiopharmaceuticalsPSMA-targeting radioligand therapyPSMA-targeting radioligands