General Information of This Metabolic Reaction (MR) (ID: MR001427)
Formula
CYP3A4 ...
SVG example
O-Dealkylation
Reactant Lapatinib ditosylate Product O-dealkylated lapatinib
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A4 (CYP3A4) DME Info
Cytochrome P450 2C8 (CYP2C8) DME Info
Metabolic Type Oxidation - O-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
MR001430 Lapatinib ditosylate GW42393 Unclear Lapatinib ditosylate [1]
MR001431 Lapatinib ditosylate GW690006 Unclear Lapatinib ditosylate [1]
MR001428 Lapatinib ditosylate N-dealkylated lapatinib Oxidation - N-Dealkylation Lapatinib ditosylate [1]
MR001429 Lapatinib ditosylate N-hydroxy lapatinib Oxidation - N-Hydroxylation Lapatinib ditosylate [1]
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
MR001424 Lapatinib ditosylate metabolite M1 Lapatinib ditosylate metabolite M1-glucuronide conjugate Conjugation - Glucuronidation Lapatinib ditosylate [2], [3], [2]
MR001425 Lapatinib ditosylate metabolite M1 Lapatinib ditosylate metabolite M1-sulfate conjugate Conjugation - Sulfation Lapatinib ditosylate [2], [3], [2]
MR001426 Lapatinib ditosylate metabolite M1 Lapatinib ditosylate metabolite M3 Oxidation - Oxidation Lapatinib ditosylate [2], [3], [2]
MR001418 O-dealkylated lapatinib Reactive Quinoneimine metabolite Unclear Lapatinib ditosylate [1]
References
1 Metabolic intermediate complex formation of human cytochrome P450 3A4 by lapatinib Drug Metab Dispos. 2011 Jun;39(6):1022-30. doi: 10.1124/dmd.110.037531.
2 Detoxication versus Bioactivation Pathways of Lapatinib In Vitro: UGT1A1 Catalyzes the Hepatic Glucuronidation of Debenzylated Lapatinib Drug Metab Dispos. 2021 Mar;49(3):233-244. doi: 10.1124/dmd.120.000236.
3 Case Study 11: Considerations for Enzyme Mapping Experiments-Interaction Between the Aldehyde Oxidase Inhibitor Hydralazine and Glutathione. Methods Mol Biol. 2021;2342:809-823. doi: 10.1007/978-1-0716-1554-6_30.

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