Title : In Vitro Metabolism of Montelukast by Cytochrome P450s and UDP-Glucuronosyltransferases.

Pub. Date : 2015 Dec

PMID : 26374173






3 Functional Relationships(s)
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1 Montelukast has been recommended as a selective in vitro and in vivo probe of cytochrome P450 (P450) CYP2C8 activity, but its selectivity toward this enzyme remains unclear. montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens
2 Kinetic and inhibition experiments performed at therapeutically relevant concentrations reveal that CYP2C8 and CYP2C9 are the principal enzymes responsible for montelukast 36-hydroxylation to 1,2-diol. montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens
3 The utility of montelukast as a probe of CYP2C8 activity may be compromised owing to involvement of multiple P450s and UGT1A3 in its metabolism. montelukast cytochrome P450 family 2 subfamily C member 8 Homo sapiens