Title : Evaluation of 6β-hydroxycortisol, 6β-hydroxycortisone, and a combination of the two as endogenous probes for inhibition of CYP3A4 in vivo.

Pub. Date : 2011 Jun

PMID : 21490593






2 Functional Relationships(s)
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1 The aim of this study was to determine whether formation clearance (CL(f)) of the sum of 6beta-hydroxycortisol and 6beta-hydroxycortisone is a useful probe of CYP3A4 inhibition in vivo. 6 beta-hydroxycortisone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 In human liver microsomes (HLMs), the formation of 6beta-hydroxycortisol and 6beta-hydroxycortisone was catalyzed by CYP3A4, and itraconazole inhibited these reactions with half maximal inhibitory concentration (IC(50))(,u) values of 3.1 nmol/l and 3.4 nmol/l, respectively. 6 beta-hydroxycortisone cytochrome P450 family 3 subfamily A member 4 Homo sapiens