放射性核素示踪技术在化学创新药人体物质平衡中的应用

Application of Radionuclide Tracer Technique in The Body Balance of Chemical Innovative Drugs

在化学创新药的研发过程中,低能量放射性核素(主要为14C)示踪技术可用于开展人体物质平衡研究,以明确用药后一定时间内药物及其代谢物的主要排泄途径(尿液还是粪便)及排泄回收率(需>90%)。该技术在创新药人体吸收、代谢及排泄研究中仍具有其他技术无法比拟的优势,在日本及欧美制药工业界已被广泛应用多年。本文简述放射性核素示踪的基本原理,回顾2018年以来在美国批准的新分子实体新药中应用该技术的情况,阐述放射性核素示踪技术在人体物质平衡研究中的应用及其在我国创新药研发中的前景。

In the research and development of chemical innovative drugs,low-energy radionuclide(mainly C14)tracer technology can be used to carry out research on the human body's material balance to clarify the drugs and their metabolites about the main excretion pathways(urine or feces)and excretion recovery rate(need to be>90%)in a certain period of time.This technology still has unparalleled advantages in the study of the absorption,metabolism and excretion of innovative drugs in human body,and it has been widely used in Japan,Europe and the United States pharmaceutical industry for many years.This article briefly describes the basic principles of radionuclide tracing,reviews the application of this technology in new molecular entities and new drugs approved in the United States since 2018,and describes the application of radionuclide tracing technology in the study of human body's balance and its prospect in the research and development of innovative drugs in China.