General Information of This Metabolic Reaction (MR) (ID: MR000905)
Formula Reactant Efavirenz Product Efavirenz metabolite M2
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 Metabolize 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]
MR000904 Efavirenz Efavirenz metabolite M5 Oxidation - Hydroxylation Efavirenz [5]
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 Clinical pharmacokinetics and drug-drug interactions of Elbasvir/Grazoprevir. Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):509-531.

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