Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR004671)
Formula Reactant Imatinib mesylate Product Piperidine N-oxide imatinib
Reactant Info Product Info
Metabolic Enzyme Dimethylaniline oxidase 3 (FMO3) DME Info
Cytochrome P450 3A4 (CYP3A4) DME Info
Metabolic Type Oxidation - N-4 oxidation
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
MR004670 Imatinib mesylate AFN911 Oxidation - Benzyl hydroxylation Imatinib mesylate [1]
MR004677 Imatinib mesylate APG049 imatinib Oxidation - Oxidationn Imatinib mesylate [2]
MR004676 Imatinib mesylate APG050 imatinib Oxidation - Oxidationn Imatinib mesylate [2]
MR004667 Imatinib mesylate Deaminated imatinib Multi-steps Reaction - Oxidationn deamination; carboxylation Imatinib mesylate [2]
MR004675 Imatinib mesylate M28.8 imatinib Oxidation - Oxidationn Imatinib mesylate [2]
MR004674 Imatinib mesylate M29.6 imatinib Oxidation - Oxidationn Imatinib mesylate [2]
MR004673 Imatinib mesylate M7 N-oxidation imatinib Oxidation - N-oxidation Imatinib mesylate [1]
MR004669 Imatinib mesylate N-Desmethylimatinib Oxidation - N-demethylation Imatinib mesylate [3], [4], [1]
MR004672 Imatinib mesylate Pyridine N-oxide imatinib Oxidation - N-oxidation Imatinib mesylate [1]
MR004668 Imatinib mesylate M42.2 imatinib Multi-steps Reaction - Oxidationn deamination; carboxylation Imatinib mesylate [2]
References
1 In vitro biotransformation of imatinib by the tumor expressed CYP1A1 and CYP1B1
2 Metabolism and disposition of imatinib mesylate in healthy volunteers
3 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
4 Participation of CYP2C8 and CYP3A4 in the N-demethylation of imatinib in human hepatic microsomes

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