Lau Joseph, Rousseau Etienne, Kwon Daniel, Lin Kuo-Shyan, Bénard François, Chen Xiaoyuan
Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA.
Department of Nuclear Medicine and Radiobiology, University of Sherbrooke, Sherbrooke, QC J1H 5N4, Canada.
Cancers (Basel). 2020 May 21;12(5):1312. doi: 10.3390/cancers12051312.
While the development of positron emission tomography (PET) radiopharmaceuticals closely follows that of traditional drug development, there are several key considerations in the chemical and radiochemical synthesis, preclinical assessment, and clinical translation of PET radiotracers. As such, we outline the fundamentals of radiotracer design, with respect to the selection of an appropriate pharmacophore. These concepts will be reinforced by exemplary cases of PET radiotracer development, both with respect to their preclinical and clinical evaluation. We also provide a guideline for the proper selection of a radionuclide and the appropriate labeling strategy to access a tracer with optimal imaging qualities. Finally, we summarize the methodology of their evaluation in in vitro and animal models and the road to clinical translation. This review is intended to be a primer for newcomers to the field and give insight into the workflow of developing radiopharmaceuticals.
虽然正电子发射断层扫描（PET）放射性药物的开发紧跟传统药物开发的步伐，但在PET放射性示踪剂的化学和放射化学合成、临床前评估及临床转化方面，仍有几个关键的注意事项。因此，我们概述了放射性示踪剂设计的基本原理，涉及合适药效基团的选择。PET放射性示踪剂开发的示例案例，无论是临床前评估还是临床评估，都将强化这些概念。我们还提供了一份指南，用于正确选择放射性核素和合适的标记策略，以获得具有最佳成像质量的示踪剂。最后，我们总结了在体外和动物模型中对它们进行评估的方法以及临床转化的途径。这篇综述旨在为该领域的新手提供入门指导，并深入了解放射性药物的开发流程。
