| Title | Quantitative relationship between rifampicin exposure and induction of Cyp3a11 in SXR humanized mice: extrapolation to human CYP3A4 induction potential. | | Author(s) | Kim S, Pray D, Zheng M, Morgan DG, Pizzano JG, Zoeckler ME, Chimalakonda A, Sinz MW | | Institution | Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb, Wallingford, CT 06492, USA. sean.kim@bms.com | | Source | Drug Metab Lett 2008 Aug; 2(3):169-75. | | Abstract | The SXR humanized mouse model was used to quantitatively assess an in vivo induction response of the human PXR agonist, rifampicin. Three days of rifampicin treatment increased RNA expression and microsomal enzyme activity of CYP3A11, as well as significantly reduced triazolam plasma exposure. These results indicate that the humanized SXR mouse can be used as a model to predict human CYP3A4 induction and the resulting pharmacokinetic changes of CYP3A4 substrates in humans. | | Language | eng | | Pub Type(s) | Journal Article
| | PubMed ID | 19356089 |
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