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ZHU Sang, ZHANG Feng, GAO Shouhong, WANG Zhipeng, CHEN Wangsheng, TAO Xia. Research progress of in vivo biomarkers for CYP3A enzyme[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(5): 385-388,402. doi: 10.3969/j.issn.1006-0111.2016.05.001
Citation: ZHU Sang, ZHANG Feng, GAO Shouhong, WANG Zhipeng, CHEN Wangsheng, TAO Xia. Research progress of in vivo biomarkers for CYP3A enzyme[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(5): 385-388,402. doi: 10.3969/j.issn.1006-0111.2016.05.001

Research progress of in vivo biomarkers for CYP3A enzyme

doi: 10.3969/j.issn.1006-0111.2016.05.001
  • Received Date: 2015-12-30
  • Rev Recd Date: 2016-03-15
  • Human cytochrome P450 (CYP) 3A, which is widely involved in the various drug metabolism, is most abundant in liver and intestine. The activity of CYP3A enzyme may be induced or inhibited in the process of drug metabolisms, and affect the metabolism of other CYP3A substrates and modulators vice versa. At present, in vitro probe drugs and in vivo biomarkers are both available to evaluate the activity of CYP3A enzyme. The former requires oral probe drugs, the latter does not need for those drugs and just allows laboratory technicians to detect endogenous substrates, such as 4β-hydroxycholesterol and 6β-hydroxycortisol. As reported, studies on CYP3A help to explain the inter-individually variability in drug metabolism, to indicate dose adjustments in combination regimens when drug interactions exist, to predict drug efficacy and toxicity reaction for providing theoretical guidance for individualized medication, and to reduce market risk of new drugs for the potential drug interactions. We summarized these two kinds of endogenous biomarkers and their clinical application in this review.
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Research progress of in vivo biomarkers for CYP3A enzyme

doi: 10.3969/j.issn.1006-0111.2016.05.001

Abstract: Human cytochrome P450 (CYP) 3A, which is widely involved in the various drug metabolism, is most abundant in liver and intestine. The activity of CYP3A enzyme may be induced or inhibited in the process of drug metabolisms, and affect the metabolism of other CYP3A substrates and modulators vice versa. At present, in vitro probe drugs and in vivo biomarkers are both available to evaluate the activity of CYP3A enzyme. The former requires oral probe drugs, the latter does not need for those drugs and just allows laboratory technicians to detect endogenous substrates, such as 4β-hydroxycholesterol and 6β-hydroxycortisol. As reported, studies on CYP3A help to explain the inter-individually variability in drug metabolism, to indicate dose adjustments in combination regimens when drug interactions exist, to predict drug efficacy and toxicity reaction for providing theoretical guidance for individualized medication, and to reduce market risk of new drugs for the potential drug interactions. We summarized these two kinds of endogenous biomarkers and their clinical application in this review.

ZHU Sang, ZHANG Feng, GAO Shouhong, WANG Zhipeng, CHEN Wangsheng, TAO Xia. Research progress of in vivo biomarkers for CYP3A enzyme[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(5): 385-388,402. doi: 10.3969/j.issn.1006-0111.2016.05.001
Citation: ZHU Sang, ZHANG Feng, GAO Shouhong, WANG Zhipeng, CHEN Wangsheng, TAO Xia. Research progress of in vivo biomarkers for CYP3A enzyme[J]. Journal of Pharmaceutical Practice and Service, 2016, 34(5): 385-388,402. doi: 10.3969/j.issn.1006-0111.2016.05.001
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