Reaction: Imatinib to 1 product

Reaction
Reaction type
N-demethylation
Direction
Major circulating metabolite?
Yes
Spontaneous?
No
Activity
active
References
  1. 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]
  2. 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]
  3. 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
EnzymeKmVmaxRole
Cytochrome P450 2C9Not AvailableNot Availableconfirmed
Cytochrome P450 3A5Not AvailableNot Availableconfirmed
Cytochrome P450 2D6Not AvailableNot Availableconfirmed
Cytochrome P450 1A2Not AvailableNot Availableconfirmed
Cytochrome P450 3A4Not AvailableNot Availableconfirmed
Cytochrome P450 2C8Not AvailableNot Availableconfirmed
Cytochrome P450 1A1Not AvailableNot Availableconfirmed
Leukotriene-B(4) omega-hydroxylase 1Not AvailableNot Availableconfirmed