Prostate cancer ranks second among the causes of death of malignant tumors in middle-aged and elderly men. A considerable number of patients are not easily detected in early-stage prostate cancer. Although traditional imaging examinations are of high value in the diagnosis and staging of prostate cancer, they also have certain limitations. With the development of nuclear medicine instruments and molecular probes, molecular imaging is playing an increasingly important role in the diagnosis and treatment of prostate cancer. Positron emission tomography and computed tomography (PET/CT) using prostate-specific membrane antigen (PSMA) as a probe has gained increasing recognition. This article will review the latest progress in the application of PET/CT using probes for targeting PSMA to imaging and treatment of prostate cancer, in order to provide a theoretical basis for the application of probes for targeting PSMA in the diagnosis and treatment of prostate cancer.