Title : Contribution of itraconazole metabolites to inhibition of CYP3A4 in vivo.

Pub. Date : 2008 Jan

PMID : 17495874






3 Functional Relationships(s)
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1 Contribution of itraconazole metabolites to inhibition of CYP3A4 in vivo. Itraconazole cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 A 3.9-fold decrease in the hepatic intrinsic clearance of a CYP3A4 substrate was predicted using the average unbound steady-state concentrations (C(ss,ave,u)) and liver microsomal inhibition constants for ITZ, OH-ITZ, keto-ITZ, and ND-ITZ. Itraconazole cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Accounting for circulating metabolites of ITZ significantly improved the in vitro to in vivo extrapolation of CYP3A4 inhibition compared to a consideration of ITZ exposure alone. Itraconazole cytochrome P450 family 3 subfamily A member 4 Homo sapiens