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：
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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.
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