{"title":"[177Lu]Lu-IBA作为骨缓解候选药物的人体吸收剂量评价。","authors":"Hassan Ranjbar, Zahra Pourhabib","doi":"10.1055/a-1486-3683","DOIUrl":null,"url":null,"abstract":"<p><p>The role of lutetium-177 among bone-seeking radionuclides in targeted therapy is noteworthy. The clinical pharmacokinetics of ibandronate (IBA) indicates that this bisphonate has powerful bone mineral affinity. The aim of this study was to evaluate of [<sup>177</sup>Lu]Lu-IBA efficacy as a new compound.The [<sup>177</sup>Lu]Lu-IBA was prepared by radiolabeling of IBA ligand to <sup>177</sup>LuCl3 that was obtained by thermal neutron irradiation of enriched Lu2O3 sample. Produced [<sup>177</sup>Lu]Lu-IBA with high radiochemical purity was administered intravenously to mice. Biodistribution data were collected at 1, 4, 24, 48 h and 7 d post injections. With calculating accumulated activities in each organ and extrapolating mouse's organs to human's organs by the RADAR method and using OLINDA/EXM software the injected dose in various human organs was achieved.[<sup>177</sup>Lu]Lu-IBA was produced with radiochemical purity nearly 96 %. Its biodistribution data showed the high uptake and durability in the skeletal tissues without significant uptake in other major organs.The results showed that [<sup>177</sup>Lu]Lu-IBA has considerably good properties as a bone-seeking radiopharmaceutical and therefore can be a candidate for bone pain palliative therapy in skeletal metastases; however, further biological studies are still needed.</p>","PeriodicalId":19238,"journal":{"name":"Nuklearmedizin-nuclear Medicine","volume":"60 5","pages":"375-380"},"PeriodicalIF":1.0000,"publicationDate":"2021-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Human Absorbed Dose Evaluation of [177Lu]Lu-IBA as a Bone Palliative Candidate.\",\"authors\":\"Hassan Ranjbar, Zahra Pourhabib\",\"doi\":\"10.1055/a-1486-3683\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>The role of lutetium-177 among bone-seeking radionuclides in targeted therapy is noteworthy. The clinical pharmacokinetics of ibandronate (IBA) indicates that this bisphonate has powerful bone mineral affinity. The aim of this study was to evaluate of [<sup>177</sup>Lu]Lu-IBA efficacy as a new compound.The [<sup>177</sup>Lu]Lu-IBA was prepared by radiolabeling of IBA ligand to <sup>177</sup>LuCl3 that was obtained by thermal neutron irradiation of enriched Lu2O3 sample. Produced [<sup>177</sup>Lu]Lu-IBA with high radiochemical purity was administered intravenously to mice. Biodistribution data were collected at 1, 4, 24, 48 h and 7 d post injections. With calculating accumulated activities in each organ and extrapolating mouse's organs to human's organs by the RADAR method and using OLINDA/EXM software the injected dose in various human organs was achieved.[<sup>177</sup>Lu]Lu-IBA was produced with radiochemical purity nearly 96 %. Its biodistribution data showed the high uptake and durability in the skeletal tissues without significant uptake in other major organs.The results showed that [<sup>177</sup>Lu]Lu-IBA has considerably good properties as a bone-seeking radiopharmaceutical and therefore can be a candidate for bone pain palliative therapy in skeletal metastases; however, further biological studies are still needed.</p>\",\"PeriodicalId\":19238,\"journal\":{\"name\":\"Nuklearmedizin-nuclear Medicine\",\"volume\":\"60 5\",\"pages\":\"375-380\"},\"PeriodicalIF\":1.0000,\"publicationDate\":\"2021-10-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Nuklearmedizin-nuclear Medicine\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1055/a-1486-3683\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2021/6/8 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q4\",\"JCRName\":\"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Nuklearmedizin-nuclear Medicine","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1055/a-1486-3683","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2021/6/8 0:00:00","PubModel":"Epub","JCR":"Q4","JCRName":"RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING","Score":null,"Total":0}
Human Absorbed Dose Evaluation of [177Lu]Lu-IBA as a Bone Palliative Candidate.
The role of lutetium-177 among bone-seeking radionuclides in targeted therapy is noteworthy. The clinical pharmacokinetics of ibandronate (IBA) indicates that this bisphonate has powerful bone mineral affinity. The aim of this study was to evaluate of [177Lu]Lu-IBA efficacy as a new compound.The [177Lu]Lu-IBA was prepared by radiolabeling of IBA ligand to 177LuCl3 that was obtained by thermal neutron irradiation of enriched Lu2O3 sample. Produced [177Lu]Lu-IBA with high radiochemical purity was administered intravenously to mice. Biodistribution data were collected at 1, 4, 24, 48 h and 7 d post injections. With calculating accumulated activities in each organ and extrapolating mouse's organs to human's organs by the RADAR method and using OLINDA/EXM software the injected dose in various human organs was achieved.[177Lu]Lu-IBA was produced with radiochemical purity nearly 96 %. Its biodistribution data showed the high uptake and durability in the skeletal tissues without significant uptake in other major organs.The results showed that [177Lu]Lu-IBA has considerably good properties as a bone-seeking radiopharmaceutical and therefore can be a candidate for bone pain palliative therapy in skeletal metastases; however, further biological studies are still needed.
期刊介绍:
Als Standes- und Fachorgan (Organ von Deutscher Gesellschaft für Nuklearmedizin (DGN), Österreichischer Gesellschaft für Nuklearmedizin und Molekulare Bildgebung (ÖGN), Schweizerischer Gesellschaft für Nuklearmedizin (SGNM, SSNM)) von hohem wissenschaftlichen Anspruch befasst sich die CME-zertifizierte Nuklearmedizin/ NuclearMedicine mit Diagnostik und Therapie in der Nuklearmedizin und dem Strahlenschutz: Originalien, Übersichtsarbeiten, Referate und Kongressberichte stellen aktuelle Themen der Diagnose und Therapie dar.
Ausführliche Berichte aus den DGN-Arbeitskreisen, Nachrichten aus Forschung und Industrie sowie Beschreibungen innovativer technischer Geräte, Einrichtungen und Systeme runden das Konzept ab.
Die Abstracts der Jahrestagungen dreier europäischer Fachgesellschaften sind Bestandteil der Kongressausgaben.
Nuklearmedizin erscheint regelmäßig mit sechs Ausgaben pro Jahr und richtet sich vor allem an Nuklearmediziner, Radiologen, Strahlentherapeuten, Medizinphysiker und Radiopharmazeuten.