Abstract: Prostate cancer is one of the most common cancers. High morbidity and mortality make it a significant threat to men’s health. Nowadays, standard diagnostic technologies could not provide effective and accurate imaging for early-stage prostate cancer. PET/CT and SPECT/CT could be used for early diagnosis of prostate cancer. Prostate-specific membrane antigen(PSMA) is widely overexpressed on the surface of prostate cancer cells, and it is an ideal target for the imaging and therapy of prostate cancer. This review first introduces the incidence of prostate cancer and current standard diagnostic methods and then describes the basic structure of PSMA and the interaction mechanism between PSMA and antibody or small molecule inhibitors. Next, it focuses on the research status and progress of diagnostic radiopharmaceuticals based on PSMA, especially emphasizing on ⁹⁹Tc^m, ⁶⁸Ga and ¹⁸F radiopharmaceuticals. In the end, the trend of PSMA targeting diagnostic radiopharmaceuticals is discussed.