Reaction: Chloroquine to 1 product

Reaction
Reaction type
N-dealkylation
Direction
Major circulating metabolite?
Yes
Spontaneous?
No
Activity
active
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
  2. Kaewkhao K, Chotivanich K, Winterberg M, Day NP, Tarning J, Blessborn D: High sensitivity methods to quantify chloroquine and its metabolite in human blood samples using LC-MS/MS. Bioanalysis. 2019 Mar;11(5):333-347. doi: 10.4155/bio-2018-0202. Epub 2019 Mar 15. [PubMed:30873854]
  3. Kim KA, Park JY, Lee JS, Lim S: Cytochrome P450 2C8 and CYP3A4/5 are involved in chloroquine metabolism in human liver microsomes. Arch Pharm Res. 2003 Aug;26(8):631-7. [PubMed:12967198]
  4. Li XQ, Bjorkman A, Andersson TB, Gustafsson LL, Masimirembwa CM: Identification of human cytochrome P(450)s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data. Eur J Clin Pharmacol. 2003 Sep;59(5-6):429-42. Epub 2003 Aug 12. [PubMed:12920490]
  5. Projean D, Baune B, Farinotti R, Flinois JP, Beaune P, Taburet AM, Ducharme J: In vitro metabolism of chloroquine: identification of CYP2C8, CYP3A4, and CYP2D6 as the main isoforms catalyzing N-desethylchloroquine formation. Drug Metab Dispos. 2003 Jun;31(6):748-54. [PubMed:12756207]
  6. Ducharme J, Farinotti R: Clinical pharmacokinetics and metabolism of chloroquine. Focus on recent advancements. Clin Pharmacokinet. 1996 Oct;31(4):257-74. doi: 10.2165/00003088-199631040-00003. [PubMed:8896943]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
Cytochrome P450 2C8Not AvailableNot Availableconfirmed
Cytochrome P450 2D6Not AvailableNot Availableconfirmed
Cytochrome P450 3A4Not AvailableNot Availableconfirmed
Cytochrome P450 3A5Not AvailableNot Availableconfirmed