Fully Automated Production and Characterization of 64Cu and Proof‐of‐Principle Small‐Animal PET Imaging Using 64Cu‐Labelled CA XII Targeting 6A10 Fab,ChemMedChem

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Fully Automated Production and Characterization of 64Cu and Proof‐of‐Principle Small‐Animal PET Imaging Using 64Cu‐Labelled CA XII Targeting 6A10 Fab
ChemMedChem ( IF 3.6 ) Pub Date : 2018-05-23 , DOI: 10.1002/cmdc.201800130
Luise Fiedler ₁ , Markus Kellner ₂ , Rosel Oos ₁ , Guido Böning ₁ , Sibylle Ziegler ₁ , Peter Bartenstein ₁ , Reinhard Zeidler _{2,

3} , Franz Josef Gildehaus ₁ , Simon Lindner ₁

Affiliation

⁶⁴Cu is a cyclotron‐produced radionuclide which offers, thanks to its characteristic decay scheme, the possibility of combining positron emission tomography (PET) investigations with radiotherapy. We evaluated the Alceo system from Comecer SpA to automatically produce ⁶⁴Cu for radiolabelling purposes. We established a ⁶⁴Cu production routine with high yields and radionuclide purity in combination with excellent operator radiation protection. The carbonic anhydrase XII targeting 6A10 antibody Fab fragment was successfully radiolabelled with the produced ⁶⁴Cu, and proof‐of‐principle small‐animal PET experiments on mice bearing glioma xenografts were performed. We obtained a high tumor‐to‐contralateral muscle ratio, which encourages further in vivo investigations of the radioconjugate regarding a possible application in diagnostic tumor imaging.

中文翻译：

全自动生产和表征64Cu和原理验证的小动物PET成像，使用针对6A10 Fab的64Cu钟形CA XII

⁶⁴ Cu是回旋加速器产生的放射性核素，由于其特有的衰变方案，它提供了将正电子发射断层扫描（PET）研究与放射疗法相结合的可能性。我们对Comecer SpA的Alceo系统进行了评估，以自动产生⁶⁴ Cu进行放射性标记。我们建立了具有高收率和放射性核素纯度以及出色的操作员辐射防护能力的⁶⁴ Cu生产程序。靶向6A10抗体Fab片段的碳酸酐酶XII成功地用产生的⁶⁴进行了铜和原则证明的小动物PET实验，对带有神经胶质瘤异种移植物的小鼠进行了实验。我们获得了很高的肿瘤与对侧肌肉比例，这鼓励了放射性结合物的进一步体内研究，以探讨其在诊断性肿瘤成像中的可能应用。

更新日期：2018-05-23

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