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

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

Volume: 2 Issue: 3

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

Affiliation:

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

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.

Cite this article as:

Kim Sean, Pray Devin, Zheng Ming, Morgan G. Danial, Pizzano G. Jenifer, Zoeckler E. Mary, Chimalakonda Anjaneya and Sinz W. Michael, Quantitative Relationship Between Rifampicin Exposure and Induction of CYP3a11 in SXR Humanized Mice: Extrapolation to Human CYP3A4 Induction Potential, Drug Metabolism Letters 2008; 2 (3) . https://dx.doi.org/10.2174/187231208785425809