Drug Metabolism Letters

Zhiyang Zhao
Amgen
Cambridge, MA
USA

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Quantitative Relationship Between Rifampicin Exposure and Induction of CYP3a11 in SXR Humanized Mice: Extrapolation to Human CYP3A4 Induction Potential

Author(s): Sean Kim, Devin Pray, Ming Zheng, Danial G. Morgan, Jenifer G. Pizzano, Mary E. Zoeckler, Anjaneya Chimalakonda, Michael W. Sinz.

Abstract:

The SXR humanized mouse modle was used to quantitatively assess an vivo induction response of the human PXR agoinst, rifampicin, Three days of rifampicin treatment increased RNA expression and microsomel enzyme activity of CYP3A, as wall as significantly reduced triazolam plasma exposure. These results indicate that the humanized SXR mouse can be used as a modle to prediict human CYP3A4 induction and the resulting pharma cokinetic changes of CYP3A4 substrates in humans.

Keywords: CYP induction, SXR-humanized mouse, rifampicin, drug-drug interaction, CYP3A4, CYP3A11

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Article Details

VOLUME: 2
ISSUE: 3
Year: 2008
Page: [169 - 175]
Pages: 7
DOI: 10.2174/187231208785425809
Price: $58