Prostate‐Specific Membrane Antigen (PSMA)‐Targeted Radionuclide Probes for Imaging and Therapy of Prostate Cancer

Abstract Prostate cancer (PCa) is one of the common cancers among men. Despite the prevalence of PCa, there are still unmet medical needs in the diagnosis and treatment of metastatic prostate cancer. Prostate‐specific membrane antigen (PSMA) is a type II zinc‐dependent metalloprotease which is highly overexpressed in metastatic PCa. In the last several years, PCa imaging probes targeting PSMA have been developed in academia as well as in industry. Among them, low molecular weight PSMA‐targeted ligands based on the Glu‐urea‐Lys scaffold have been evaluated in preclinical and clinical studies. This review provides an overview of the recent development in PSMA‐targeted imaging or therapeutic probes for metastatic PCa.