Background: Prostate cancer (PCa) is the most common sex-related malignancy with high
mortality in men worldwide. Prostate-specific membrane antigen (PSMA) is overexpressed on the surface
of most prostate tumor cells and considered a valuable target for both the diagnosis and therapy of
prostate cancer. A series of radiolabeled agents have been developed based on the featured PSMA
ligands in the previous decade and have demonstrated promising outcomes in clinical research of primary
and recurrent PCa. Furthermore, the inspiring response and safety of lutetium-177-PSMA (177Lu-
PSMA) radiotherapy represent the potential for expanded therapeutic options for metastatic castrationresistant
PCa. Retrospective cohort studies have revealed that radiolabeled PSMA agents are the mainstays
of the current success, especially in detecting prostate cancer with metastasis and biochemical recurrence.
Objective: This review is intended to present a comprehensive overview of the current literature on
PSMA ligand-based agents for both radionuclide imaging and therapeutic approaches, with a focus on
those that have been clinically adopted.
Conclusion: PSMA-based diagnosis and therapy hold great promise for improving the clinical management
of prostate cancer.