Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR001124)
Formula
SVG example
5-Hydroxylation
Reactant Gemfibrozil Product Gemfibrozil metabolite M1
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A4 (CYP3A4) DME Info
Metabolic Type Oxidation - 5-Hydroxylation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR001125 Gemfibrozil Gemfibrozil 1-beta-glucuronide metabolite Conjugation - O-Glucuronidation Gemfibrozil [1], [2], [3]
MR001126 Gemfibrozil Gemfibrozil metabolite M2 Oxidation - 4-Hydroxylation Gemfibrozil [4], [5], [6]
MR001127 Gemfibrozil Gemfibrozil metabolite M4 Unclear Gemfibrozil [7], [5]
Other MR(s) Related to The Product of This MR
Other MR(s) That Metabolize The Produtc of This MR
MR ID Reactant Product MR Type Related Drug REF
MR001123 Gemfibrozil metabolite M1 Gemfibrozil metabolite M3 Unclear Gemfibrozil [8], [5], [6]
References
1 Intracellular pharmacokinetics of gemcitabine, its deaminated metabolite 2',2'-difluorodeoxyuridine and their nucleotides Br J Clin Pharmacol. 2018 Jun;84(6):1279-1289. doi: 10.1111/bcp.13557.
2 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
3 The UDP-glucuronosyltransferase 2B7 isozyme is responsible for gemfibrozil glucuronidation in the human liver. Drug Metab Dispos. 2007 Nov;35(11):2040-4.
4 Congenital Zika syndrome in non-endemic regions J Perinat Med. 2018 Sep 25;46(7):819. doi: 10.1515/jpm-2017-0403.
5 Biodegradation of emerging organic pollutant gemfibrozil: Mechanism, kinetics and pathway modelling. Bioresour Technol. 2023 Apr;374:128749. doi: 10.1016/j.biortech.2023.128749.
6 Metabolic Activation of Gemfibrozil Mediated by Cytochrome P450 Enzymes and Sulfotransferases. Chem Res Toxicol. 2022 Jul 18;35(7):1257-1266. doi: 10.1021/acs.chemrestox.2c00054.
7 Gemfibrozil metabolite inhibits in vitro low-density lipoprotein (LDL) oxidation and diminishes cytotoxicity induced by oxidized LDL Metabolism. 2000 Apr;49(4):479-85. doi: 10.1016/s0026-0495(00)80012-8.
8 Clinical pharmacokinetics of fibric acid derivatives (fibrates). Clin Pharmacokinet. 1998 Feb;34(2):155-62.

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