Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR000898)
Formula
SVG example
Hydroxylation
Reactant 8-hydroxy-efavirenz Product Efavirenz metabolite M8
Reactant Info Product Info
Metabolic Type Oxidation - Hydroxylation
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
MR000899 8-hydroxy-efavirenz Efavirenz metabolite M1 Conjugation - Conjugation Efavirenz [5], [6]
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
MR000900 Efavirenz metabolite M8 Efavirenz metabolite M14 Conjugation - Conjugation 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.
6 The Activity of Members of the UDP-Glucuronosyltransferase Subfamilies UGT1A and UGT2B is Impaired in Patients with Liver Cirrhosis. Clin Pharmacokinet. 2023 Jun 16. doi: 10.1007/s40262-023-01261-3.

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