Precision medication based on the evaluation of drug metabolizing enzyme and transporter functions

Yanrong Ma , Jing Mu , Xueyan Gou , Xinan Wu

Precision Clinical Medicine ›› 2025, Vol. 8 ›› Issue (1) : pbaf004

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Precision Clinical Medicine ›› 2025, Vol. 8 ›› Issue (1) :pbaf004 DOI: 10.1093/pcmedi/pbaf004
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Precision medication based on the evaluation of drug metabolizing enzyme and transporter functions

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Abstract

Pharmacogenomics, therapeutic drug monitoring, and the assessments of hepatic and renal function have made significant contributions to the advancement of individualized medicine. However, their lack of direct correlation with protein abundance/non-genetic factors, target drug concentration, and drug metabolism/excretion significantly limits their application in precision drug therapy. The primary task of precision medicine is to accurately determine drug dosage, which depends on a precise assessment of the ability to handle drugs in vivo, and drug metabolizing enzymes and transporters are critical determinants of drug disposition in the body. Therefore, accurately evaluating the functions of these enzymes and transporters is key to assessing the capacity to handle drugs and predicting drug concentrations in target organs. Recent advancements in the evaluation of enzyme and transporter functions using exogenous probes and endogenous biomarkers show promise in advancing personalized medicine. This article aims to provide a comprehensive overview of the latest research on markers used for the functional evaluation of drug-metabolizing enzymes and transporters. It also explores the application of marker omics in systematically assessing their functions, thereby laying a foundation for advancing precision pharmacotherapy.

Keywords

precision medicine / drug metabolizing enzyme / drug transporter / probe / biomarker

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Yanrong Ma, Jing Mu, Xueyan Gou, Xinan Wu. Precision medication based on the evaluation of drug metabolizing enzyme and transporter functions. Precision Clinical Medicine, 2025, 8(1): pbaf004 DOI:10.1093/pcmedi/pbaf004

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Acknowledgements

This research was supported by the National Natural Science Foundation of China (Grant No. U21A20424) and the Natural Science Foundation of Gansu Province, China (Grant No. 24JRRA912).

Author contributions

Yanrong Ma (Funding acquisition, Visualization, Writing—original draft), Jing Mu (Writing—original draft), Xueyan Gou (Writing—original draft, Writing—review & editing) and Xinan Wu (Conceptualization, Funding acquisition, Supervision, Writing—review & editing)

Conflict of interest

None declared.

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