PSMA-Targeting Radioligand Therapy in Prostate Cancer

Radioligand therapy targeting prostate-specific membrane antigen (PSMA) represents a significant advancement in the treatment of metastatic prostate cancer. This theranostic approach involves the use of diagnostic radiotracers that specifically bind to PSMA, such as ^68^Ga-PSMA-11, to identify PSMA-positive disease. Therapeutically, radioligands such as ^177^Lutetium-PSMA-617 have shown promise for delivering targeted radiation to PSMA-expressing tumor cells. This review summarizes recent findings from key clinical trials, focusing on the state-of-the-art in radioligand therapy and optimal patient selection, as well as dosing of radionuclide therapy in special situations, including diffuse bone marrow involvement and renal toxicity. PEER REVIEWED ARTICLE Peer reviewers: PD Dr Aurelius Omlin, Onkozentrum Zurich, Zurich, Switzerland Dr Ole Maas, HOCH Health Ostschweiz, St. Gallen, Switzerland Dr Marco Cuzzocrea, Cantonal Hospital Bellinzona (EOC), Bellinzona, Switzerland Received on November 11, 2024; accepted after peer review on December 19, 2024; published online on December 27, 2024.