对有机光氧化还原反应产生的 [18F]FDOPA 的首次人体评估。
First-in-Human Evaluation of [18F]FDOPA Produced by Organo-Photoredox Reactions.
发表日期:2024 Jul 18
作者:
Li Wang, Zhiyu Lv, Liping Yang, Xuedan Wu, Yan Zhu, Lin Liu, Yan Zhao, Zhanwen Huang, David A Nicewicz, Zhanhong Wu, Yue Chen, Zibo Li
来源:
BIOCONJUGATE CHEMISTRY
摘要:
光氧化还原是有机化学中强大的合成工具,已广泛应用于核医学和分子成像等各个领域。特别是,基于吖啶的有机光氧化还原放射性标记极大地影响了正电子发射断层扫描(PET)试剂的生产和发现。尽管在临床前研究中得到广泛应用,但通过吖啶光氧化还原标记合成的 PET 试剂尚未在人体中进行过测试。 [18F]FDOPA在临床上用于肿瘤诊断和神经精神疾病的评估,但其应用受到复杂的合成方法、需要昂贵的模块和/或消耗材料/盒的高成本的限制。在本报告中,我们将光氧化还原标记单元与自动化模块集成,并生产了用于人类研究的[18F]FDOPA。这项研究不仅代表了对吖啶类有机光氧化还原反应生成的 PET 试剂的首次人体研究,而且证明了这种新型标记方法的安全性,为该技术生成的其他 PET 试剂的临床转化提供了里程碑/参考。未来。
Photoredox is a powerful synthetic tool in organic chemistry and has been widely used in various fields, including nuclear medicine and molecular imaging. In particular, acridinium-based organophotoredox radiolabeling has significantly impacted the production and discovery of positron emission tomography (PET) agents. Despite their extensive use in preclinical research, no PET agents synthesized by acridinium photoredox labeling have been tested in humans. [18F]FDOPA is clinically used for tumor diagnosis and the evaluation of neuropsychiatric disorders, but its application is limited by complex synthesis methods, the need for expensive modules, and/or the high cost of consumable materials/cassettes. In this report, we integrated a photoredox labeling unit with an automated module and produced [18F]FDOPA for human study. This research not only represents the first human study of a PET agent generated by acridinium-based organophotoredox reactions but also demonstrates the safety of this novel labeling method, serving as a milestone/reference for the clinical translation of other PET agents generated by this technique in the future.