Abstract: Prostate-specific membrane antigen (PSMA), highly expressed in prostate cancer, provides a new strategy for the clinical diagnosis and treatment of prostate cancer as a specific biological target. At present, the research on the labeling of  PSMA small molecule inhibitors is mostly focused on positron nuclide labels, such as ⁶⁸Ga and ¹⁸F or beta radionuclide labels, such as ¹⁷⁷Lu to realize diagnosis and targeted therapy of prostate cancer. In recent years, the application of single photon nuclide-labeled PSMA small molecule inhibitors has also made progress. This review summarizes the clinical application of single photon nuclide-labeled PSMA small molecule inhibitors in prostate cancer.