Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR001279)
Formula
SVG example
N-Dealkylation
Reactant Itraconazole Product N-desalkyl-itraconazole
Reactant Info Product Info
Metabolic Type Oxidation - N-Dealkylation
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
MR001277 Itraconazole Hydroxyitraconazole Oxidation - O-Demethylation Itraconazole [1], [2], [3], [4], [5]
MR001278 Itraconazole Keto-itraconazole Unclear Itraconazole [1], [2]
References
1 Role of itraconazole metabolites in CYP3A4 inhibition. Drug Metab Dispos. 2004 Oct;32(10):1121-31.
2 Accurate prediction of dose-dependent CYP3A4 inhibition by itraconazole and its metabolites from in vitro inhibition data Clin Pharmacol Ther. 2010 Oct;88(4):499-505. doi: 10.1038/clpt.2010.119.
3 Repurposing antifungals: population pharmacokinetics of itraconazole and hydroxy-itraconazole following administration of a nanocrystal formulation. J Antimicrob Chemother. 2023 May 3;78(5):1219-1224. doi: 10.1093/jac/dkad072.
4 Does metabolite matter? Defining target itraconazole and hydroxy-itraconazole serum concentrations for blastomycosis. Mycoses. 2023 May;66(5):412-419. doi: 10.1111/myc.13565.
5 Influence of Gender, Body Mass Index, and Age on the Pharmacokinetics of Itraconazole in Healthy Subjects: Non-Compartmental Versus Compartmental Analysis. Front Pharmacol. 2022 Jun 15;13:796336. doi: 10.3389/fphar.2022.796336.

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