Reaction: Clozapine to 1 product
- Reaction
- Reaction type
- N-oxidation
- Direction
- Major circulating metabolite?
- No
- Spontaneous?
- No
- Activity
- unknown
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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
Enzyme Km Vmax Role Cytochrome P450 3A4 Not Available Not Available implied Cytochrome P450 1A2 Not Available Not Available implied Dimethylaniline monooxygenase [N-oxide-forming] 3 Not Available Not Available implied Cytochrome P450 2C19 Not Available Not Available confirmed Cytochrome P450 3A5 Not Available Not Available confirmed Cytochrome P450 2D6 Not Available Not Available confirmed Cytochrome P450 2C9 Not Available Not Available confirmed Cytochrome P450 2E1 Not Available Not Available implied