PSMA ligand

PSMA ligands are a class of small molecules or peptidomimetics designed to target prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II, which is highly overexpressed on the surface of prostate cancer cells and in the neovasculature of various other solid tumors. These ligands typically consist of a glutamate-urea-glutamate or glutamate-urea-lysine binding motif that selectively binds to the active site of PSMA. They are widely utilized as targeting vectors in theranostic applications, where they are conjugated to diagnostic radionuclides (such as Gallium-68 or Fluorine-18) for positron emission tomography (PET) imaging, or to therapeutic radionuclides (such as Lutetium-177 or Actinium-225) to deliver targeted radiation directly to tumor cells. Additionally, they can be conjugated to fluorophores for intraoperative tumor visualization or to cytotoxic payloads as drug conjugates.

Other names

prostate-specific membrane antigen ligandPSMA inhibitorPSMA ligandsPSMA-targeted ligandPSMA-targeting agentPSMA-targeting ligand