225 Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic.

Autor: Rubira L; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, France., Deshayes E; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, France.; Institut de Recherche en Cancérologie de Montpellier (IRCM), INSERM U1194, University Montpellier, Institut Régional du Cancer de Montpellier (ICM), 34298 Montpellier, France., Santoro L; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, France.; Institut de Recherche en Cancérologie de Montpellier (IRCM), INSERM U1194, University Montpellier, Institut Régional du Cancer de Montpellier (ICM), 34298 Montpellier, France., Kotzki PO; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, France.; Institut de Recherche en Cancérologie de Montpellier (IRCM), INSERM U1194, University Montpellier, Institut Régional du Cancer de Montpellier (ICM), 34298 Montpellier, France., Fersing C; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, France.; IBMM, University Montpellier, CNRS, ENSCM, 34293 Montpellier, France.
Jazyk: angličtina
Zdroj: Pharmaceutics [Pharmaceutics] 2023 Mar 24; Vol. 15 (4). Date of Electronic Publication: 2023 Mar 24.
DOI: 10.3390/pharmaceutics15041051
Abstrakt: The widespread use of peptide receptor radionuclide therapy (PRRT) represents a major therapeutic breakthrough in nuclear medicine, particularly since the introduction of 177 Lu-radiolabeled somatostatin analogs. These radiopharmaceuticals have especially improved progression-free survival and quality of life in patients with inoperable metastatic gastroenteropancreatic neuroendocrine tumors expressing somatostatin receptors. In the case of aggressive or resistant disease, the use of somatostatin derivatives radiolabeled with an alpha-emitter could provide a promising alternative. Among the currently available alpha-emitting radioelements, actinium-225 has emerged as the most suitable candidate, especially regarding its physical and radiochemical properties. Nevertheless, preclinical and clinical studies on these radiopharmaceuticals are still few and heterogeneous, despite the growing momentum for their future use on a larger scale. In this context, this report provides a comprehensive and extensive overview of the development of 225 Ac-labeled somatostatin analogs; particular emphasis is placed on the challenges associated with the production of 225 Ac, its physical and radiochemical properties, as well as the place of 225 Ac-DOTATOC and 225 Ac-DOTATATE in the management of patients with advanced metastatic neuroendocrine tumors.
Databáze: MEDLINE
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