Prostate Cancer Radioligand Therapy: PSMA and Beyond, Current Landscape and Future Directions

There has been a rapid increase in the use and investigation of radioligand therapies for prostate cancer. This review summarizes and synthesizes the current prostate cancer radioligand landscape. It highlights the challenges facing optimal radioligand use and outlines approaches to improve the efficacy of this therapeutic class.

The prostate specific membrane antigen (PSMA)-directed radioligand ¹⁷⁷Lu-PSMA-617 improves survival in patients with metastatic castrate resistant prostate cancer (mCRPC) after chemotherapy and is now a standard of care treatment option for these patients. Published and ongoing trials promise to expand the use of radioligand therapies in prostate cancer. These trials highlight the potential of novel radioligand targets, alternate radioisotopes, and combination therapy approaches to improve radioligand efficacy. Emerging radioligands, novel combination therapies, optimized patient selection, and dose-personalization promise to improve outcomes and expand the use of radioligand therapies in prostate cancer.