Application progress of radiolabeling strategies in human mass balance studies
10.16438/j.0513-4870.2024-0378
- VernacularTitle:放射性同位素标记策略在人体物质平衡试验中的应用进展
- Author:
Yi-fei HE
1
;
Yuan-dong ZHENG
2
;
Da-fang ZHONG
2
;
Xing-xing DIAO
1
Author Information
1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; University of Chinese Academy of Sciences, Beijing 101408, China
2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
- Publication Type:Research Article
- Keywords:
mass balance;
radiolabeling;
isotope tracing technology;
rug metabolism;
human radioactive trials
- From:
Acta Pharmaceutica Sinica
2024;59(9):2470-2483
- CountryChina
- Language:Chinese
-
Abstract:
Human mass balance study is a pivotal research in the field of clinical pharmacology, aiming at elucidating the metabolic and excretion pathways of drugs in humans. Currently, human mass balance studies predominantly employ radiolabeling techniques. Recently, both the U.S. Food and Drug Administration (FDA) and the Center for Drug Evaluation (CDE) of the China National Medical Products Administration (NMPA) issued related research drafts and guidelines to encourage and guide the pharmaceutical industry to conduct research in compliance with established standards. The selection of radiolabeling sites is crucial for obtaining critical information on drug metabolism. However, in vivo biotransformation may lead to partial disintegration of the molecular structure, thereby resulting in the loss of metabolic product information of the unlabeled moiety. Administering drugs with different radiolabeling sites separately or in combination, or labeling multiple radioactive isotopes within one molecule, can effectively solve this problem. This article reviews relevant technological progress, analyzes radiolabeling strategies, and discusses the application of drugs with multiple radiolabeling sites in human mass balance studies.
