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PSMA-Targeting Radiopharmaceuticals for Prostate Cancer Therapy: Recent Developments and Future Perspectives
Mohamed El Fakiri1,2,3, Nicolas M Geis1,2,3, Nawal Ayada1,2
1Department of Nuclear Medicine, University Medical Center Freiburg, Faculty of Medicine, University of Freiburg, Hugstetter Str. 55, 79106 Freiburg, Germany.
Abstract:
Prostate cancer (PC) is the second most common cancer among men, with 1.3 million yearly cases worldwide. Among those cancer-afflicted men, 30% will develop metastases and some will progress into metastatic castration-resistant prostate cancer (mCRPC), which is associated with a poor prognosis and median survival time that ranges from nine to 13 months. Nevertheless, the discovery of prostate specific membrane antigen (PSMA), a marker overexpressed in the majority of prostatic cancerous tissue, revolutionised PC care. Ever since, PSMA-targeted radionuclide therapy has gained remarkable international visibility in translational oncology. Furthermore, on first clinical application, it has shown significant influence on therapeutic management and patient care in metastatic and hormone-refractory prostate cancer, a disease that previously had remained immedicable. In this article, we provide a general overview of the main milestones in the development of ligands for PSMA-targeted radionuclide therapy, ranging from the firstly developed monoclonal antibodies to the current state-of-the-art low molecular weight entities conjugated with various radionuclides, as well as potential future efforts related to PSMA-targeted radionuclide therapy.
Insights
Prostate cancer (PC) treatment advanced with prostate specific membrane antigen (PSMA) targeted radionuclide therapy. This approach offers new hope for patients with metastatic castration-resistant prostate cancer (mCRPC).
Area of Science:
- Oncology
- Nuclear Medicine
- Translational Research
Background:
- Prostate cancer (PC) is a leading cause of cancer death in men, with a significant portion developing metastatic castration-resistant prostate cancer (mCRPC).
- mCRPC presents a poor prognosis with limited treatment options and short survival times.
- The discovery of prostate specific membrane antigen (PSMA) as a highly expressed marker in PC tissue has been a significant breakthrough.
Purpose of the Study:
- To provide an overview of the development of ligands for PSMA-targeted radionuclide therapy.
- To highlight the evolution from monoclonal antibodies to small molecule ligands.
- To discuss the current state and future directions of PSMA-targeted radionuclide therapy in PC care.
Main Methods:
- Review of historical and current literature on PSMA-targeted radionuclide therapy development.
- Analysis of the progression of ligand design, from antibodies to small molecules.
- Examination of radionuclide conjugation strategies and their clinical impact.
Main Results:
- PSMA-targeted radionuclide therapy has revolutionized the management of advanced PC, particularly mCRPC.
- The development of low molecular weight PSMA-targeting ligands has improved therapeutic efficacy and patient outcomes.
- Clinical applications have demonstrated significant influence on therapeutic strategies for previously immedicable PC.
Conclusions:
- PSMA-targeted radionuclide therapy represents a major advancement in prostate cancer treatment.
- Continued research into novel ligands and radionuclides holds promise for further improving patient care.
- This therapeutic modality offers a new avenue for managing advanced and refractory prostate cancer.
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