177LU-PSMA-617 in the treatment of castration-resistant prostate cancer: 2021-2025 review

Abstract

The continuous development of radiopharmaceuticals has expanded the therapeutic possibilities of molecular radiotherapy, with 177Lu-PSMA-617 standing out as one of the main innovations in nuclear medicine. Indicated for the treatment of metastatic castration-resistant prostate cancer (CPMRC), the radiopharmaceutical was approved by the U.S. Food and Drug Administration (FDA) in 2022, establishing itself as an effective option for patients refractory to conventional therapies. Since its introduction, clinical studies have confirmed the therapeutic potential previously observed in preclinical research, demonstrating significant benefits in both overall survival and patient quality of life. This study presents a systematic review of publications related to the use of 177Lu-PSMA-617 in the treatment of mCRPC between 2021 and July 31, 2025. The main findings, methodologies, and reported outcomes were analyzed and organized, providing a comprehensive overview of the evolution of therapy with this radiolabeled molecule. In addition to reviewing clinical efficacy, the study discusses the relevance of 177Lu as a therapeutic radionuclide and its multiple applications in molecular labeling, highlighting perspectives for the development of novel compounds. Thus, this paper offers a knowledge base for researchers and healthcare professionals, supporting both clinical practice and the advancement of scientific investigations in the field of molecular radiotherapy.