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Application progress of radiolabeling strategies in human mass balance studies
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Yi-fei HE1, 2, Yuan-dong ZHENG1, Da-fang ZHONG1, *, Xing-xing DIAO1, 2, *
Acta Pharmaceutica Sinica | 2024, 59(9) : 2470 - 2483
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Acta Pharmaceutica Sinica | 2024, 59(9): 2470-2483
Application progress of radiolabeling strategies in human mass balance studies
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Yi-fei HE1, 2, Yuan-dong ZHENG1, Da-fang ZHONG1, *, Xing-xing DIAO1, 2, *
Affiliations
  • 1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
  • 2. University of Chinese Academy of Sciences, Beijing 101408, China
Published: 2024-09-12 doi: 10.16438/j.0513-4870.2024-0378
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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.

mass balance  /  radiolabeling  /  isotope tracing technology  /  drug metabolism  /  human radioactive trials
Yi-fei HE, Yuan-dong ZHENG, Da-fang ZHONG, Xing-xing DIAO. Application progress of radiolabeling strategies in human mass balance studies[J]. Acta Pharmaceutica Sinica, 2024 , 59 (9) : 2470 -2483 . DOI: 10.16438/j.0513-4870.2024-0378
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Article Info
doi: 10.16438/j.0513-4870.2024-0378
  • Receive Date：2024-04-18
  • Online Date：2025-11-24
  • Published：2024-09-12
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  • Received：2024-04-18
  • Revised：2024-06-23
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    1. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
    2. University of Chinese Academy of Sciences, Beijing 101408, China
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表12种不同金属材料的力学参数
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Family		 属数
Number of
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Number of
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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