IVIVE (in vitro to in vivo extrapolation,体外-体内外推法)(2)

2、对于CYP3A4的底物，高清除率的化合物微粒体与肝细胞的差异明显；低清除率的化合物差异较小；

3、即使CYP3A4底物采用肝微粒体预测的误差相比于肝细胞较低（5.19 for hepatocytes and

3.47 for microsomes），但仍然处于较高的水平，个人常在推算后取3作为校正因子；

4、对于CYP1A2的底物发现采用肝微粒体和肝细胞预测的准确性均较高。

VX: DMPK

Reference：

1. IChristine M Bowman and Leslie Z. Benet (2019) In Vitro - In Vivo Accuracy: The CYP3A4 Anomaly. Drug Metabolism and Disposition September 24 2019 dmd.119.088427; DOI:

https://http://www.77cn.com.cn/10.1124/dmd.119.088427

2. Lam JL and Benet LZ (2004) Hepatic microsome studies are insufficient to characterize in vivo hepatic metabolic clearance and metabolic drug-drug interactions: studies of digoxin metabolism in primary rat hepatocytes versus microsomes. Drug Metab Dispos 32:1311-1316.