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Clinical Pharmacokinetics
Published in: Clinical Pharmacokinetics 5/2021

01-05-2021 | Review Article

Drug-Metabolizing Cytochrome P450 Enzymes Have Multifarious Influences on Treatment Outcomes

Authors: Yurong Song, Chenxi Li, Guangzhi Liu, Rui Liu, Youwen Chen, Wen Li, Zhiwen Cao, Baosheng Zhao, Cheng Lu, Yuanyan Liu

Published in: Clinical Pharmacokinetics | Issue 5/2021

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Abstract

Drug metabolism is a critical process for the removal of unwanted substances from the body. In humans, approximately 80% of oxidative metabolism and almost 50% of the overall elimination of commonly used drugs can be attributed to one or more of various cytochrome P450 (CYP) enzymes from CYP families 1–3. In addition to the basic metabolic effects for elimination, CYP enzymes in vivo are capable of affecting the treatment outcomes in many cases. Drug-metabolizing CYP enzymes are mainly expressed in the liver and intestine, the two principal drug oxidation and elimination organs, where they can significantly influence the drug action, safety, and bioavailability by mediating phase I metabolism and first-pass metabolism. Furthermore, CYP-mediated local drug metabolism in the sites of action may also have the potential to impact drug response, according to the literature in recent years. This article underlines the ability of CYP enzymes to influence treatment outcomes by discussing CYP-mediated diversified drug metabolism in primary metabolic sites (liver and intestine) and typical action sites (brain and tumors) according to their expression levels and metabolic activity. Moreover, intrinsic and extrinsic factors of personal differential CYP phenotypes that contribute to interindividual variation of treatment outcomes are also reviewed to introduce the multifarious pivotal role of CYP-mediated metabolism and clearance in drug therapy.
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Metadata
Title
Drug-Metabolizing Cytochrome P450 Enzymes Have Multifarious Influences on Treatment Outcomes
Authors
Yurong Song
Chenxi Li
Guangzhi Liu
Rui Liu
Youwen Chen
Wen Li
Zhiwen Cao
Baosheng Zhao
Cheng Lu
Yuanyan Liu
Publication date
01-05-2021
Publisher
Springer International Publishing
Published in
Clinical Pharmacokinetics / Issue 5/2021
Print ISSN: 0312-5963
Electronic ISSN: 1179-1926
DOI
https://doi.org/10.1007/s40262-021-01001-5

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