<sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic
The widespread use of peptide receptor radionuclide therapy (PRRT) represents a major therapeutic breakthrough in nuclear medicine, particularly since the introduction of <sup>177</sup>Lu-radiolabeled somatostatin analogs. These radiopharmaceuticals have especially improved progression-f...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-03-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/4/1051 |
| _version_ | 1827744027670216704 |
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| author | Léa Rubira Emmanuel Deshayes Lore Santoro Pierre Olivier Kotzki Cyril Fersing |
| author_facet | Léa Rubira Emmanuel Deshayes Lore Santoro Pierre Olivier Kotzki Cyril Fersing |
| author_sort | Léa Rubira |
| collection | DOAJ |
| description | The widespread use of peptide receptor radionuclide therapy (PRRT) represents a major therapeutic breakthrough in nuclear medicine, particularly since the introduction of <sup>177</sup>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 <sup>225</sup>Ac-labeled somatostatin analogs; particular emphasis is placed on the challenges associated with the production of <sup>225</sup>Ac, its physical and radiochemical properties, as well as the place of <sup>225</sup>Ac–DOTATOC and <sup>225</sup>Ac–DOTATATE in the management of patients with advanced metastatic neuroendocrine tumors. |
| first_indexed | 2024-03-11T04:38:04Z |
| format | Article |
| id | doaj.art-35384b5d6d394af0aad607e3fe005dcc |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T04:38:04Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-35384b5d6d394af0aad607e3fe005dcc2023-11-17T20:52:01ZengMDPI AGPharmaceutics1999-49232023-03-01154105110.3390/pharmaceutics15041051<sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to ClinicLéa Rubira0Emmanuel Deshayes1Lore Santoro2Pierre Olivier Kotzki3Cyril Fersing4Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, FranceNuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, FranceNuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, FranceNuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, FranceNuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University Montpellier, 34090 Montpellier, FranceThe widespread use of peptide receptor radionuclide therapy (PRRT) represents a major therapeutic breakthrough in nuclear medicine, particularly since the introduction of <sup>177</sup>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 <sup>225</sup>Ac-labeled somatostatin analogs; particular emphasis is placed on the challenges associated with the production of <sup>225</sup>Ac, its physical and radiochemical properties, as well as the place of <sup>225</sup>Ac–DOTATOC and <sup>225</sup>Ac–DOTATATE in the management of patients with advanced metastatic neuroendocrine tumors.https://www.mdpi.com/1999-4923/15/4/1051actinium-225radionuclide productionradiolabelingtargeted radionuclide therapytargeted alpha-therapyradiobiology |
| spellingShingle | Léa Rubira Emmanuel Deshayes Lore Santoro Pierre Olivier Kotzki Cyril Fersing <sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic Pharmaceutics actinium-225 radionuclide production radiolabeling targeted radionuclide therapy targeted alpha-therapy radiobiology |
| title | <sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic |
| title_full | <sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic |
| title_fullStr | <sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic |
| title_full_unstemmed | <sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic |
| title_short | <sup>225</sup>Ac-Labeled Somatostatin Analogs in the Management of Neuroendocrine Tumors: From Radiochemistry to Clinic |
| title_sort | sup 225 sup ac labeled somatostatin analogs in the management of neuroendocrine tumors from radiochemistry to clinic |
| topic | actinium-225 radionuclide production radiolabeling targeted radionuclide therapy targeted alpha-therapy radiobiology |
| url | https://www.mdpi.com/1999-4923/15/4/1051 |
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