<sup>212</sup>Pb: Production Approaches and Targeted Therapy Applications
Over the last decade, targeted alpha therapy has demonstrated its high effectiveness in treating various oncological diseases. Lead-212, with a convenient half-life of 10.64 h, and daughter alpha-emitter short-lived <sup>212</sup>Bi (<i>T<sub>1/2</sub></i> = 1 h),...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-01-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/1/189 |
| _version_ | 1797491074310078464 |
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| author | Konstantin V. Kokov Bayirta V. Egorova Marina N. German Ilya D. Klabukov Michael E. Krasheninnikov Antonius A. Larkin-Kondrov Kseniya A. Makoveeva Michael V. Ovchinnikov Maria V. Sidorova Dmitry Y. Chuvilin |
| author_facet | Konstantin V. Kokov Bayirta V. Egorova Marina N. German Ilya D. Klabukov Michael E. Krasheninnikov Antonius A. Larkin-Kondrov Kseniya A. Makoveeva Michael V. Ovchinnikov Maria V. Sidorova Dmitry Y. Chuvilin |
| author_sort | Konstantin V. Kokov |
| collection | DOAJ |
| description | Over the last decade, targeted alpha therapy has demonstrated its high effectiveness in treating various oncological diseases. Lead-212, with a convenient half-life of 10.64 h, and daughter alpha-emitter short-lived <sup>212</sup>Bi (<i>T<sub>1/2</sub></i> = 1 h), provides the possibility for the synthesis and purification of complex radiopharmaceuticals with minimum loss of radioactivity during preparation. As a benefit for clinical implementation, it can be milked from a radionuclide generator in different ways. The main approaches applied for these purposes are considered and described in this review, including chromatographic, solution, and other techniques to isolate <sup>212</sup>Pb from its parent radionuclide. Furthermore, molecules used for lead’s binding and radiochemical features of preparation and stability of compounds labeled with <sup>212</sup>Pb are discussed. The results of preclinical studies with an estimation of therapeutic and tolerant doses as well as recently initiated clinical trials of targeted radiopharmaceuticals are presented. |
| first_indexed | 2024-03-10T00:42:36Z |
| format | Article |
| id | doaj.art-68c463dfc4e94c738e1f3e02e41019c6 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T00:42:36Z |
| publishDate | 2022-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-68c463dfc4e94c738e1f3e02e41019c62023-11-23T15:05:20ZengMDPI AGPharmaceutics1999-49232022-01-0114118910.3390/pharmaceutics14010189<sup>212</sup>Pb: Production Approaches and Targeted Therapy ApplicationsKonstantin V. Kokov0Bayirta V. Egorova1Marina N. German2Ilya D. Klabukov3Michael E. Krasheninnikov4Antonius A. Larkin-Kondrov5Kseniya A. Makoveeva6Michael V. Ovchinnikov7Maria V. Sidorova8Dmitry Y. Chuvilin9Physical and Chemical Technology Center, National Research Center Kurchatov Institute, 123182 Moscow, RussiaDepartment of Chemistry, Lomonosov Moscow State University, 119991 Moscow, RussiaPhysical and Chemical Technology Center, National Research Center Kurchatov Institute, 123182 Moscow, RussiaDepartment of Regenerative Medicine, National Medical Research Radiological Center, 249036 Obninsk, RussiaResearch and Educational Resource Center for Cellular Technologies, Peoples’ Friendship University of Russia, 117198 Moscow, RussiaPhysical and Chemical Technology Center, National Research Center Kurchatov Institute, 123182 Moscow, RussiaPhysical and Chemical Technology Center, National Research Center Kurchatov Institute, 123182 Moscow, RussiaLaboratory of Peptide Synthesis, National Medical Research Center of Cardiology, 121552 Moscow, RussiaLaboratory of Peptide Synthesis, National Medical Research Center of Cardiology, 121552 Moscow, RussiaPhysical and Chemical Technology Center, National Research Center Kurchatov Institute, 123182 Moscow, RussiaOver the last decade, targeted alpha therapy has demonstrated its high effectiveness in treating various oncological diseases. Lead-212, with a convenient half-life of 10.64 h, and daughter alpha-emitter short-lived <sup>212</sup>Bi (<i>T<sub>1/2</sub></i> = 1 h), provides the possibility for the synthesis and purification of complex radiopharmaceuticals with minimum loss of radioactivity during preparation. As a benefit for clinical implementation, it can be milked from a radionuclide generator in different ways. The main approaches applied for these purposes are considered and described in this review, including chromatographic, solution, and other techniques to isolate <sup>212</sup>Pb from its parent radionuclide. Furthermore, molecules used for lead’s binding and radiochemical features of preparation and stability of compounds labeled with <sup>212</sup>Pb are discussed. The results of preclinical studies with an estimation of therapeutic and tolerant doses as well as recently initiated clinical trials of targeted radiopharmaceuticals are presented.https://www.mdpi.com/1999-4923/14/1/189lead-212thorium-228radionuclide generatorα-radiation sourcestargeted alpha therapy |
| spellingShingle | Konstantin V. Kokov Bayirta V. Egorova Marina N. German Ilya D. Klabukov Michael E. Krasheninnikov Antonius A. Larkin-Kondrov Kseniya A. Makoveeva Michael V. Ovchinnikov Maria V. Sidorova Dmitry Y. Chuvilin <sup>212</sup>Pb: Production Approaches and Targeted Therapy Applications Pharmaceutics lead-212 thorium-228 radionuclide generator α-radiation sources targeted alpha therapy |
| title | <sup>212</sup>Pb: Production Approaches and Targeted Therapy Applications |
| title_full | <sup>212</sup>Pb: Production Approaches and Targeted Therapy Applications |
| title_fullStr | <sup>212</sup>Pb: Production Approaches and Targeted Therapy Applications |
| title_full_unstemmed | <sup>212</sup>Pb: Production Approaches and Targeted Therapy Applications |
| title_short | <sup>212</sup>Pb: Production Approaches and Targeted Therapy Applications |
| title_sort | sup 212 sup pb production approaches and targeted therapy applications |
| topic | lead-212 thorium-228 radionuclide generator α-radiation sources targeted alpha therapy |
| url | https://www.mdpi.com/1999-4923/14/1/189 |
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