Prostate cancer is one of the most common malignant tumors among men worldwide，posing a significant threat to male health. Since prostate-specific membrane antigen（PSMA）has been proved to be the preferred biomarker for the diagnosis of prostate cancer，PSMA-targeted radiopharmaceuticals have made significant progress in the diagnosis and therapy of prostate cancer，effectively improving the diagnostic sensitivity and treatment effect of prostate cancer. This article reviews the research progress of PSMA-targeted radioactive molecular probes in recent years，analyzes the design concepts of probe structure and summarizes the clinical experience. It is expected to benefit the development of radioactive molecular probes for diagnosis and treatment of prostate cancer.