Article
Measurement and compartmental modeling of the effect of CYP3A5 gene variation on systemic and intrarenal tacrolimus disposition.
Clinical pharmacology and therapeutics - 1 Dec 2012
Zheng S, Tasnif Y, Hebert M F, Davis C L, Shitara Y, Calamia J C, Lin Y S, Shen D D, Thummel K E
Abstract excerpt
We evaluated the hypothesis that cytochrome P450 3A5 (CYP3A5) expression can affect intrarenal tacrolimus accumulation. Tacrolimus was administered orally to 24 healthy volunteers who were selected on the basis of their CYP3A5 genotype. As compared with CYP3A5 nonexpressors, expressors had a 1.6-fold higher oral tacrolimus clearance and 2.0- to 2.7-fold higher metabolite/parent area under the curve (AUC) ratios...
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