Which concentration of the inhibitor should be used to predict in vivo drug interactions from in vitro data?

被引：0

作者：

Kiyomi Ito

Koji Chiba

Masato Horikawa

Michi Ishigami

Naomi Mizuno

Jun Aoki

Yasumasa Gotoh

Takafumi Iwatsubo

Shin-ichi Kanamitsu

Motohiro Kato

Iichiro Kawahara

Kayoko Niinuma

Akiko Nishino

Norihito Sato

Yuko Tsukamoto

Kaoru Ueda

Tomoo Itoh

Yuichi Sugiyama

机构：

[1] Kitasato University,School of Pharmaceutical Sciences

[2] The University of Tokyo,Pharmacia

[3] The University of Tokyo,Nissan Chemical Industries, Ltd

[4] The University of Tokyo,Sankyo Co, Ltd

[5] The University of Tokyo,Mitsubishi

[6] The University of Tokyo,Tokyo Pharmaceuticals, Inc

[7] The University of Tokyo,Mitsui Pharmaceuticals Inc

[8] The University of Tokyo,Kissei Pharmaceutical Co, Ltd

[9] The University of Tokyo,Yamanouchi Pharmaceutical Co, Ltd

[10] The University of Tokyo,Otsuka Pharmaceutical Factory, Inc

[11] The University of Tokyo,Chugai Pharmaceutical Co, Ltd

[12] The University of Tokyo,Bayer Yakuhin Ltd

[13] The University of Tokyo,Daiichi Pharmaceutical Co, Ltd

[14] The University of Tokyo,Nippon Boehringer Ingelheim Co, Ltd

[15] The University of Tokyo,Shionogi & Co, Ltd

[16] The University of Tokyo,Nippon Roche KK

[17] The University of Tokyo,Teikoku Hormone Mfg Co, Ltd

来源：

AAPS PharmSci | / 4卷

关键词：

Drug interaction; metabolism; quantitative prediction;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

When the metabolism of a drug is competitively or noncompetitively inhibited by another drug, the degree of in vivo interaction can be evaluated from the [I]u/Ki ratio, where [I]u is the unbound concentration around the enzyme and Ki is the inhibition constant of the inhibitor. In the present study, we evaluated the metabolic inhibition potential of drugs known to be inhibitors or substrates of cytochrome P450 by estimating their [I]u/Ki ratio using literature data.

引用

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