[177Lu]Lu-IBA作为骨缓解候选药物的人体吸收剂量评价。

IF 1 4区 医学 Q4 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Nuklearmedizin-nuclear Medicine Pub Date : 2021-10-01 Epub Date: 2021-06-08 DOI:10.1055/a-1486-3683
Hassan Ranjbar, Zahra Pourhabib
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引用次数: 0

摘要

在寻骨放射性核素中,镥-177在靶向治疗中的作用值得注意。依班膦酸盐(IBA)的临床药代动力学表明,这种双膦酸盐具有强大的骨矿物质亲和力。本研究的目的是评价[177Lu]Lu-IBA作为一种新化合物的疗效。将富集的Lu2O3样品通过热中子辐照得到的177LuCl3与IBA配体进行放射性标记,制备了[177Lu]Lu-IBA。制备的[177Lu]Lu-IBA具有高放射化学纯度,经静脉注射给小鼠。分别于注射后1、4、24、48 h和7 d采集生物分布数据。通过RADAR法计算各器官累积活性,并将小鼠各器官外推到人体各器官,利用OLINDA/EXM软件计算出人体各器官的注射剂量。[177]Lu-IBA的放射化学纯度接近96%。其生物分布数据显示,在骨骼组织中有较高的吸收和持久性,在其他主要器官中没有明显的吸收。结果表明[177Lu]Lu-IBA作为一种寻骨放射性药物具有相当良好的性能,因此可以作为骨骼转移性骨痛缓解治疗的候选药物;然而,还需要进一步的生物学研究。
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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.

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来源期刊
CiteScore
1.70
自引率
13.30%
发文量
267
审稿时长
>12 weeks
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.
期刊最新文献
The Medical Informatics Initiative and the Network University Medicine - Perspectives for Nuclear Medicine. Combined morphologic-metabolic biomarkers from [18F]FDG-PET/CT stratify prognostic groups in low-risk NSCLC. NuklearMedizin 2024: Abstract-Einreichung bis zum 1. November geöffnet! DGN-Forschungs- und -Förderpreise Preisverleihungen
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