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Background: PET is a noninvasive imaging approach regarding the information on metabolic and functional changes of disease. Incorporate with CT or MRI, the imaging modality of PET/CT and PET/MRI are increasingly used in the diagnosis of PCa. Some of the imaging agents have been approved for clinical use such as 18F-FDG, 11C-choline, 18F-FACBC, 68Ga-PSMA-11, 18F-DCFPyL, and 18F-NaF. Other imaging agents that show promising PCa diagnostic potential are under development, e.g., Zr-89 labeled YS5 and 68Ga-RM2, targeting CD46 and GRPR, respectively. Aim: This review assessed the diagnostic performance of the tracers by literature study. Methods: A comprehensive search strategy based on articles available via the website of Uppsala university library from 2010 to March 2022. We select all the English articles associated with the discovery, preclinical study, clinical study, and the diagnostic performance evaluation of the imaging agents for further investigation. Results: PSMA-targeting imaging agents demonstrate superior diagnostic performance in both primary and recurrent prostate cancer compared with 11C-choline and 18F-FACBC, especially in patients with low PSA values. In comparison with 18F-NaF which is suitable for the detection of bone metastases, PSMA-targeting radiotracers are versatile, namely, PSMA-targeting scan is capable to detect lesions in lymph nodes, soft tissues, and bones. The limitation of PSMA-targeting images is that PSMA is not uniformly expressed on prostate cancer cells. Subsequently, the combination of two PET tracers has been investigated to overcome the obstacle. The preliminary studies also investigated the cost-effectiveness of PSMA-targeting imaging agents in high-risk prostate cancer patients. The result indicates that the use of PSMA-targeting radiopharmaceuticals is cost effected than conventional imaging modalities in high-risk PCa patients. Conclusion: PSMA-targeting imaging agents are the most versatile tracers in the detection of PCa available now. The combination use of two imaging agents could increase the detection rate. To further elucidate to what extent the PSMA-targeting imaging agents will benefit PCa patients, more investigations are needed.