利福平暴露与SXR人源化小鼠中Cyp3a11诱导之间的定量关系：外推至人CYP3A4诱导潜力
Quantitative relationship between rifampicin exposure and induction of Cyp3a11 in SXR humanized mice: extrapolation to human CYP3A4 induction potential.
作者信息
Kim Sean, Pray Devin, Zheng Ming, Morgan Daniel G, Pizzano Jennifer G, Zoeckler Mary E, Chimalakonda Anjaneya, Sinz Michael W
机构信息
Department of Metabolism and Pharmacokinetics, Bristol-Myers Squibb, Wallingford, CT 06492, USA.
出版信息
Drug Metab Lett. 2008 Aug;2(3):169-75. doi: 10.2174/187231208785425809.
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.
采用SXR人源化小鼠模型定量评估人PXR激动剂利福平的体内诱导反应。利福平治疗三天可增加CYP3A11的RNA表达和微粒体酶活性，并显著降低三唑仑的血浆暴露量。这些结果表明，人源化SXR小鼠可作为一种模型，用于预测人体中CYP3A4的诱导情况以及CYP3A4底物由此产生的药代动力学变化。
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