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How to Choose In Vitro Systems to Predict In Vivo Drug Clearance: A System Pharmacology Perspective

机译:如何选择体外系统来预测体内药物清除率:系统药理学的观点

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摘要

The use of in vitro metabolism data to predict human clearance has become more significant in the current prediction of large scale drug clearance for all the drugs. The relevant information (in vitro metabolism data and in vivo human clearance values) of thirty-five drugs that satisfied the entry criteria of probe drugs was collated from the literature. Then the performance of different in vitro systems including Escherichia coli system, yeast system, lymphoblastoid system and baculovirus system is compared after in vitro-in vivo extrapolation. Baculovirus system, which can provide most of the data, has almost equal accuracy as the other systems in predicting clearance. And in most cases, baculovirus system has the smaller CV in scaling factors. Therefore, the baculovirus system can be recognized as the suitable system for the large scale drug clearance prediction.
机译:在当前对所有药物的大规模药物清除的预测中,使用体外代谢数据来预测人清除率变得更加重要。从文献中整理了满足探针药物进入标准的35种药物的相关信息(体外代谢数据和体内人类清除率值)。然后,在体外-体内外推法之后比较了不同的体外系统的性能,包括大肠杆菌系统,酵母系统,淋巴母细胞系统和杆状病毒系统。可以提供大部分数据的杆状病毒系统在预测清除率方面具有与其他系统几乎相同的准确性。而且在大多数情况下,杆状病毒系统的缩放因子CV较小。因此,杆状病毒系统可以被认为是用于大规模药物清除率预测的合适系统。

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