〔Abstract〕 Prostate cancer is one of the most common malignant tumors of male genitourinary system. Prostate cancer has the following characteristics: insidious onset, early asymptomatic or not obvious symptoms, complex etiology and pathogenesis, long incubation period and so on.Therefore, the realization of its early diagnosis and treatment is of great significance to the prognosis of patients. Prostate-specific membrane antigen (PSMA) is a type 2 transmembrane glycoprotein that is highly expressed on the membrane of almost all primary and metastatic prostate cancer cells, and is an ideal target for prostate cancer imaging and treatment. In recent years, with the approval of urea-containing small molecule PET (positron emission computed tomography) radiopharmaceutical based on PSMA (68Ga-PSMA-11, 18F-PSMA-1007), PET-CT (positron emission computed tomography/computed tomography) has shown new potential for early diagnosis and accurate staging of prostate cancer patients. Therefore, this review mainly summarizes the research progress of urea-containing PSMA PET imaging agents and finds that they have defects such as uptake in non-target tissues like the kidneys, lacrimal glands, and salivary glands. Thus, further optimizing their structure to reduce the uptake in non-target tissues, providing provide convenience for the labeling of therapeutic radiopharmaceuticals, thereby achieving the goal of integrated diagnosis and treatment, is an important development direction in this field.