Title : CYP2C8 but not CYP3A4 is important in the pharmacokinetics of montelukast.

Pub. Date : 2012 Feb

PMID : 21838784






6 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 CYP2C8 but not CYP3A4 is important in the pharmacokinetics of montelukast. montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens
2 Our aim was to study the effects of selective CYP2C8 and CYP3A4 inhibitors on the pharmacokinetics of montelukast. montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens
3 Plasma concentrations of montelukast, gemfibrozil, itraconazole and their metabolites were measured up to 72 h. RESULTS: The CYP2C8 inhibitor gemfibrozil increased the AUC(0, ) of montelukast 4.3-fold and its t(1/2) 2.1-fold (P < 0.001). montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens
4 Plasma concentrations of montelukast, gemfibrozil, itraconazole and their metabolites were measured up to 72 h. RESULTS: The CYP2C8 inhibitor gemfibrozil increased the AUC(0, ) of montelukast 4.3-fold and its t(1/2) 2.1-fold (P < 0.001). montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens
5 CONCLUSIONS: CYP2C8 is the dominant enzyme in the biotransformation of montelukast in humans, accounting for about 80% of its metabolism. montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens
6 Montelukast may serve as a safe and useful CYP2C8 probe drug. montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens