Evaluation of F-537-Tetrazine in a model for brain pretargeting imaging. Comparison to N-(3-[18F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine

IF 3.6 4区医学 Q1 RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING Nuclear medicine and biology Pub Date : 2024-01-01 DOI:10.1016/j.nucmedbio.2024.108877

Vladimir Shalgunov , Sara Lopes van den Broek , Ida Vang Andersen , Nakul R. Raval , Gabriela Schäfer , Matthias Barz , Matthias M. Herth , Umberto M. Battisti

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Abstract

Brain pretargeted nuclear imaging for the diagnosis of various neurodegenerative diseases is a quickly developing field. The tetrazine ligation is currently the most explored approach to achieve this goal due to its remarkable properties. In this work, we evaluated the performance of F-537-Tetrazine, previously developed by Biogen, and N-(3-[¹⁸F]fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine, previously developed in our group, thereby allowing for the direct comparison of these two imaging probes. The evaluation included synthesis, radiolabeling and a comparison of the physicochemical properties of the compounds. Furthermore, their performance was evaluated by in vitro and in vivo pretargeting models. This study indicated that N-(3-[¹⁸F] fluoro-5-(1,2,4,5-tetrazin-3-yl)benzyl)propan-1-amine might be more suited for brain pretargeted imaging.

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F-537-Tetrazine 在脑部预靶向成像模型中的评估。与 N-(3-[18F]氟-5-(1,2,4,5-四嗪-3-基)苄基)丙-1-胺的比较

用于诊断各种神经退行性疾病的脑预靶向核成像是一个发展迅速的领域。由于四嗪的显著特性，它是目前实现这一目标的最常用方法。在这项工作中，我们评估了百健公司之前开发的 F-537-Tetrazine 和我们小组之前开发的 N-(3-[18F]氟-5-(1,2,4,5-四嗪-3-基)苄基)丙-1-胺的性能，从而可以直接比较这两种成像探针。评估包括化合物的合成、放射性标记和理化性质比较。此外，还通过体外和体内预靶向模型对它们的性能进行了评估。这项研究表明，N-(3-[18F] 氟-5-(1,2,4,5-四嗪-3-基)苄基)丙-1-胺可能更适合于脑预靶成像。

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来源期刊

Nuclear medicine and biology 医学-核医学

CiteScore

6.00

自引率

9.70%

发文量

479

审稿时长

51 days

期刊介绍： Nuclear Medicine and Biology publishes original research addressing all aspects of radiopharmaceutical science: synthesis, in vitro and ex vivo studies, in vivo biodistribution by dissection or imaging, radiopharmacology, radiopharmacy, and translational clinical studies of new targeted radiotracers. The importance of the target to an unmet clinical need should be the first consideration. If the synthesis of a new radiopharmaceutical is submitted without in vitro or in vivo data, then the uniqueness of the chemistry must be emphasized. These multidisciplinary studies should validate the mechanism of localization whether the probe is based on binding to a receptor, enzyme, tumor antigen, or another well-defined target. The studies should be aimed at evaluating how the chemical and radiopharmaceutical properties affect pharmacokinetics, pharmacodynamics, or therapeutic efficacy. Ideally, the study would address the sensitivity of the probe to changes in disease or treatment, although studies validating mechanism alone are acceptable. Radiopharmacy practice, addressing the issues of preparation, automation, quality control, dispensing, and regulations applicable to qualification and administration of radiopharmaceuticals to humans, is an important aspect of the developmental process, but only if the study has a significant impact on the field. Contributions on the subject of therapeutic radiopharmaceuticals also are appropriate provided that the specificity of labeled compound localization and therapeutic effect have been addressed.