PDF(Pubmed)
Abstract：
In the field of nuclear medicine, the β+ -emitting 43Sc and β- -emitting 47Sc are promising candidates in cancer diagnosis and targeted radionuclide therapy (TRT) due to their favorable decay schema and shared pharmacokinetics as a true theranostic pair. Additionally, scandium is a group-3 transition metal (like 177Lu) and exhibits affinity for DOTA-based chelators, which have been studied in depth, making the barrier to implementation lower for 43/47Sc than for other proposed true theranostics. Before 43/47Sc can see widespread pre-clinical evaluation, however, an accessible production methodology must be established and each isotope\'s radiolabeling and animal imaging capabilities studied with a widely utilized tracer. As such, a simple means of converting an 18 MeV biomedical cyclotron to support solid targets and produce 43Sc via the 42Ca(d,n)43Sc reaction has been devised, exhibiting reasonable yields. The NatTi(γ,p)47Sc reaction is also investigated along with the successful implementation of chemical separation and purification methods for 43/47Sc. The conjugation of 43/47Sc with PSMA-617 at specific activities of up to 8.94 MBq/nmol and the subsequent imaging of LNCaP-ENZaR tumor xenografts in mouse models with both 43/47Sc-PSMA-617 are also presented.
摘要：
在核医学领域，β+发射43Sc和β-发射47Sc在癌症诊断和靶向放射性核素治疗（TRT）中是有希望的候选者，因为它们具有良好的衰变模式和共享的药代动力学作为真正的治疗对。此外,钪是3族过渡金属（如177Lu），对基于DOTA的螯合剂具有亲和力，已经深入研究，使43/47Sc的实施障碍低于其他拟议的真正治疗方法。在43/47Sc之前可以看到广泛的临床前评估，然而,必须建立一种可获得的生产方法，并使用广泛使用的示踪剂研究每种同位素的放射性标记和动物成像能力。因此，一种将18MeV生物医学回旋加速器转换为支持固体靶标并通过42Ca产生43Sc的简单方法（d，N)设计了43Sc反应，表现出合理的收益率。NatTi（γ，p）47Sc反应还与成功实施43/47Sc的化学分离和纯化方法一起进行了研究。还提供了43/47Sc与PSMA-617在高达8.94MBq/nmol的比活性下的缀合以及随后在具有43/47Sc-PSMA-617的小鼠模型中LNCaP-ENZaR肿瘤异种移植物的成像。
