Reaction: Imatinib to 1 product
- Reaction
- Reaction type
- N-demethylation
- Direction
- Major circulating metabolite?
- Yes
- Spontaneous?
- No
- Activity
- active
- References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: 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. Epub 2009 Sep 1. [Article]
- Nebot N, Crettol S, d'Esposito F, Tattam B, Hibbs DE, Murray M: Participation of CYP2C8 and CYP3A4 in the N-demethylation of imatinib in human hepatic microsomes. Br J Pharmacol. 2010 Nov;161(5):1059-69. doi: 10.1111/j.1476-5381.2010.00946.x. [Article]
- Rochat B, Zoete V, Grosdidier A, von Grunigen S, Marull M, Michielin O: In vitro biotransformation of imatinib by the tumor expressed CYP1A1 and CYP1B1. Biopharm Drug Dispos. 2008 Mar;29(2):103-18. doi: 10.1002/bdd.598. [Article]
- Comments
- Not Available
- Enzymes
Enzyme Km Vmax Role Cytochrome P450 2C9 Not Available Not Available confirmed Cytochrome P450 3A5 Not Available Not Available confirmed Cytochrome P450 2D6 Not Available Not Available confirmed Cytochrome P450 1A2 Not Available Not Available confirmed Cytochrome P450 3A4 Not Available Not Available confirmed Cytochrome P450 2C8 Not Available Not Available confirmed Cytochrome P450 1A1 Not Available Not Available confirmed Leukotriene-B(4) omega-hydroxylase 1 Not Available Not Available confirmed