Research progress of in vivo biomarkers for CYP3A enzyme

VernacularTitle:CY P3 A酶内源性标志物的研究进展
Author: Sang ZHU ¹ ; Feng ZHANG ; Shouhong GAO ; Zhipeng WANG ; Wangsheng CHEN ; Xia TAO
Author Information

1. 上海长征医院药材科
Keywords: In vivo biomarkers; 4β-hydroxycholesterol; 6β-hydroxycortisol
From: Journal of Pharmaceutical Practice 2016;34(5):385-388,402
CountryChina
Language:Chinese
Abstract: Human cytochrome P450 (CYP) 3A ,which is widely involved in the various drug metabolism ,is most abun-dant 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 bio-markers are both available to evaluate the activity of CYP 3A 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 in-dicate 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 inter-actions .We summarized these two kinds of endogenous biomarkers and their clinical application in this review .