Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR001117)
Formula
CYP1A1 ...
SVG example
Oxidative Defluorination
Reactant Gefitinib Product Oxidative defluorination of the halogenated phenyl group
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 1A1 (CYP1A1) DME Info
Cytochrome P450 3A4 (CYP3A4) DME Info
Cytochrome P450 3A5 (CYP3A5) DME Info
Metabolic Type Oxidation - Oxidative Defluorination
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
MR001116 Gefitinib Desmethyl-gefitinib M523595 Oxidation - O-Demethylation Gefitinib [1], [2]
MR001115 Gefitinib Metabolism of the N-propoxymorpholino-group Unclear Gefitinib [3]
References
1 Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition Xenobiotica. 2006 Jan;36(1):29-39. doi: 10.1080/00498250500523253.
2 An investigation into possible interactions among four vascular epidermal growth factor receptor-tyrosine kinase inhibitors with gefitinib. Cancer Chemother Pharmacol. 2021 Jan;87(1):43-52. doi: 10.1007/s00280-020-04191-0.
3 Reactive metabolite of gefitinib activates inflammasomes: implications for gefitinib-induced idiosyncratic reaction J Toxicol Sci. 2020;45(11):673-680. doi: 10.2131/jts.45.673.

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