Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR000899)
Formula
UGT
SVG example
Conjugation
Reactant 8-hydroxy-efavirenz Product Efavirenz metabolite M1
Reactant Info Product Info
Metabolic Enzyme UDP-glucuronyltransferase (UGT) DME Info
Metabolic Type Conjugation - Conjugation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Produce The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000903 Efavirenz 8-hydroxy-efavirenz Oxidation - Hydroxylation Efavirenz [1], [2], [3], [4]
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000898 8-hydroxy-efavirenz Efavirenz metabolite M8 Oxidation - Hydroxylation Efavirenz [1], [5], [6]
References
1 Induction of CYP3A4 by efavirenz in primary human hepatocytes: comparison with rifampin and phenobarbital. J Clin Pharmacol. 2004 Nov;44(11):1273-81.
2 Biotransformation of Efavirenz and Proteomic Analysis of Cytochrome P450s and UDP-Glucuronosyltransferases in Mouse, Macaque, and Human Brain-Derived In Vitro Systems. Drug Metab Dispos. 2023 Apr;51(4):521-531. doi: 10.1124/dmd.122.001195.
3 Liver Cirrhosis Affects the Pharmacokinetics of the Six Substrates of the Basel?Phenotyping Cocktail Differently. Clin Pharmacokinet. 2022 Jul;61(7):1039-1055. doi: 10.1007/s40262-022-01119-0.
4 Instability of Efavirenz Metabolites Identified During Method Development and Validation. J Pharm Sci. 2021 Oct;110(10):3362-3366. doi: 10.1016/j.xphs.2021.06.028.
5 Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218.
6 Evaluation of CYP2B6 induction and prediction of clinical drug-drug interactions: considerations from the IQ consortium induction working group-an industry perspective. Drug Metab Dispos. 2016 Oct;44(10):1720-30.

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