Prostate cancer is a malignant tumor posing significant threats to the health of men worldwide. In advanced stages, it frequently progresses to castration-resistant prostate cancer, which is characterized by complex mechanisms and poor prognosis. In such cases, conventional treatments have limited effectiveness. However, the emergence of radionuclide therapy has provided new hope. Lutetium-177-labeled prostate-specific membrane antigen (177Lu-PSMA), currently the most promising radioligand in clinical research, received approval from the U.S. Food and Drug Administration (FDA) in 2022. This review comprehensively summarizes recent advancements, efficacy assessments, and safety evaluations of 177Lu-PSMA therapy. Additionally, we analyze its current limitations and suggest future research directions for PSMA-targeted radioligand therapy (RLT). Undoubtedly, 177Lu-PSMA-617 is transforming metastatic castration-resistant prostate cancer (mCRPC) treatment. However, challenges remain regarding its potential standardization for use in non-mCRPC cases, the optimal treatment sequence, standardized imaging/molecular biomarkers, and toxicity management, all of which require further prospective validation.

Keywords: 177Lu-PSMA; biomarkers; clinical trials; combination therapy; precision medicine; prostate cancer; radioligand therapy;
radiopharmaceuticals