Reaction: Clozapine to 1 product

Reaction
Reaction type
N-oxidation
Direction
Major circulating metabolite?
No
Spontaneous?
No
Activity
unknown
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. Piatkov I, Caetano D, Assur Y, Lau SL, Coelho M, Jones T, Nguyen T, Boyages S, McLean M: CYP2C19*17 protects against metabolic complications of clozapine treatment. World J Biol Psychiatry. 2017 Oct;18(7):521-527. doi: 10.1080/15622975.2017.1347712. Epub 2017 Jul 18. [Article]
  3. Toth K, Csukly G, Sirok D, Belic A, Kiss A, Hafra E, Deri M, Menus A, Bitter I, Monostory K: Potential Role of Patients' CYP3A-Status in Clozapine Pharmacokinetics. Int J Neuropsychopharmacol. 2017 Jul 1;20(7):529-537. doi: 10.1093/ijnp/pyx019. [Article]
  4. Wagmann L, Meyer MR, Maurer HH: What is the contribution of human FMO3 in the N-oxygenation of selected therapeutic drugs and drugs of abuse? Toxicol Lett. 2016 Sep 6;258:55-70. doi: 10.1016/j.toxlet.2016.06.013. Epub 2016 Jun 15. [Article]
  5. Dragovic S, Gunness P, Ingelman-Sundberg M, Vermeulen NP, Commandeur JN: Characterization of human cytochrome P450s involved in the bioactivation of clozapine. Drug Metab Dispos. 2013 Mar;41(3):651-8. doi: 10.1124/dmd.112.050484. Epub 2013 Jan 7. [Article]
  6. Zhang WV, D'Esposito F, Edwards RJ, Ramzan I, Murray M: Interindividual variation in relative CYP1A2/3A4 phenotype influences susceptibility of clozapine oxidation to cytochrome P450-specific inhibition in human hepatic microsomes. Drug Metab Dispos. 2008 Dec;36(12):2547-55. doi: 10.1124/dmd.108.023671. Epub 2008 Sep 22. [Article]
  7. Tugnait M, Hawes EM, McKay G, Rettie AE, Haining RL, Midha KK: N-oxygenation of clozapine by flavin-containing monooxygenase. Drug Metab Dispos. 1997 Apr;25(4):524-7. [Article]
  8. Pirmohamed M, Williams D, Madden S, Templeton E, Park BK: Metabolism and bioactivation of clozapine by human liver in vitro. J Pharmacol Exp Ther. 1995 Mar;272(3):984-90. [Article]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
Cytochrome P450 3A4Not AvailableNot Availableimplied
Cytochrome P450 1A2Not AvailableNot Availableimplied
Dimethylaniline monooxygenase [N-oxide-forming] 3Not AvailableNot Availableimplied
Cytochrome P450 2C19Not AvailableNot Availableconfirmed
Cytochrome P450 3A5Not AvailableNot Availableconfirmed
Cytochrome P450 2D6Not AvailableNot Availableconfirmed
Cytochrome P450 2C9Not AvailableNot Availableconfirmed
Cytochrome P450 2E1Not AvailableNot Availableimplied