Abstract: Prostate cancer (PCa) is one of the most common reasons for male death, seriously endangering human life and health. With the application of prostate specific membrane antigen PSMAtargeted radiopharmaceuticals in PET/CT and SPECT/CT, the sensitivity and accuracy of diagnosis have been efficiently improved. In this paper, we firstly introduce the core structures of PSMAtargeted small molecule drugs. Then ureabased PSMAtargeted radiopharmaceuticals (radionuclides include ⁶⁸Ga, ¹⁸F, ¹¹C, ^99mTc, ⁶⁴Cu, ¹²³I, ¹²⁵I, ¹³¹I, ¹⁷⁷Lu, ²²⁵Ac, ²¹³Bi, ²¹²Pb, etc.) and recent progress in diagnosis and therapy are highlighted. Finally, this research field is summarized and prospected.