Article
The influence of CYP3A5 expression on the extent of hepatic CYP3A inhibition is substrate-dependent: an in vitro-in vivo evaluation.
Drug metabolism and disposition: the biological fate of chemicals - 1 Jan 2008
Isoherranen Nina, Ludington Shana R, Givens Raymond C, Lamba Jatinder K, Pusek Susan N, Dees E Claire, Blough David K, Iwanaga Kazunori, Hawke Roy L, Schuetz Erin G, Watkins Paul B, Thummel Kenneth E, Paine Mary F
Abstract excerpt
Despite several studies suggesting that CYP3A5 expression can influence the extent of hepatic CYP3A-mediated inhibition, a systematic in vitro-in vivo evaluation of this potential clinically important issue has not been reported. Using representative probes from two distinct CYP3A substrate subgroups (midazolam, erythromycin), the inhibitory potency of fluconazole was evaluated in pooled human liver microsomes...
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