PSMA-Targeting Radiopharmaceuticals for Prostate Cancer Therapy: Recent Developments and Future Perspectives
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 m...
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| Veröffentlicht in: | Cancers 2021-08, Vol.13 (16), p.3967 |
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| creator | El Fakiri, Mohamed Geis, Nicolas M. Ayada, Nawal Eder, Matthias Eder, Ann-Christin |
| description | 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. |
| doi_str_mv | 10.3390/cancers13163967 |
| format | Article |
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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.</description><identifier>ISSN: 2072-6694</identifier><identifier>EISSN: 2072-6694</identifier><identifier>DOI: 10.3390/cancers13163967</identifier><identifier>PMID: 34439121</identifier><language>eng</language><publisher>Basel: MDPI AG</publisher><subject>Adenocarcinoma ; Amino acids ; Binding sites ; Biodistribution ; Cancer therapies ; Castration ; Disease management ; Drug dosages ; Glycoproteins ; Ligands ; Medical research ; Membrane proteins ; Metastases ; Metastasis ; Molecular weight ; Monoclonal antibodies ; Nuclear medicine ; Pharmacokinetics ; Prostate cancer ; Radiation therapy ; Radioisotopes ; Review ; Survival ; Tumors</subject><ispartof>Cancers, 2021-08, Vol.13 (16), p.3967</ispartof><rights>2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). 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| source | PubMed Central Open Access; MDPI - Multidisciplinary Digital Publishing Institute; EZB-FREE-00999 freely available EZB journals; PubMed Central |
| subjects | Adenocarcinoma Amino acids Binding sites Biodistribution Cancer therapies Castration Disease management Drug dosages Glycoproteins Ligands Medical research Membrane proteins Metastases Metastasis Molecular weight Monoclonal antibodies Nuclear medicine Pharmacokinetics Prostate cancer Radiation therapy Radioisotopes Review Survival Tumors |
| title | PSMA-Targeting Radiopharmaceuticals for Prostate Cancer Therapy: Recent Developments and Future Perspectives |
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