PSMA-targeting radioligands

PSMA-targeting radioligands are a class of radiopharmaceuticals designed to target prostate-specific membrane antigen (PSMA), a cell-surface protein highly overexpressed in prostate cancer, particularly in metastatic castration-resistant prostate cancer (mCRPC). These agents typically consist of a urea-based targeting ligand (such as PSMA-617 or PSMA-11) that binds with high affinity to the active site of PSMA, connected via a linker to a chelator holding a radionuclide. Depending on the radionuclide, they are used either for diagnostic imaging (e.g., gallium-68 or fluorine-18 for PET/CT) or for targeted radionuclide therapy (e.g., lutetium-177 or actinium-225). Therapeutic radioligands deliver localized, high-energy radiation directly to the tumor cells, causing DNA damage and cell death while sparing surrounding healthy tissues.

Other names

PSMA-targeted radioligandPSMA-targeted radioligandsPSMA-targeting radioligand