Gefitinib (Iressa) inhibits the CYP3A4-mediated formation of 7-ethyl-10-(4-amino-1-piperidino)carbonyloxycamptothecin but activates that of 7-ethyl-10-[4-N-(5-aminopentanoic acid)-1-piperidino] carbonyloxycamptothecin from irinotecan

被引：14

作者：

Fujita, K ^{[1
]}

Ando, Y ^{[1
]}

Narabayashi, M ^{[1
]}

Miya, T ^{[1
]}

Nagashima, F ^{[1
]}

Yamamoto, W ^{[1
]}

Kodama, K ^{[1
]}

Araki, K ^{[1
]}

Endo, H ^{[1
]}

Sasaki, Y ^{[1
]}

机构：

[1] Saitama Med Sch, Dept Clin Oncol, Moroyama, Saitama 3500495, Japan

来源：

DRUG METABOLISM AND DISPOSITION | 2005年 / 33卷 / 12期

关键词：

D O I：

10.1124/dmd.105.006205

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Gefitinib ( Iressa) is an anticancer drug that selectively inhibits tyrosine kinases of epidermal growth factor receptor. Gefitinib might affect CYP3A4-mediated metabolism, since the drug is a substrate of human CYP3A. In this study, we evaluated the effects of gefitinib on drug metabolism catalyzed by human CYP3A4. The effects of gefitinib on the CYP3A4-mediated formation of NPC (7-ethyl-10-(4-amino-1-piperidino) carbonyloxycamptothecin) and that of APC (7-ethyl-10-[4-N-(5-aminopentanoicacid)-1-piperidino] carbonyloxycamptothecin) from irinotecan were examined with the use of human liver and small intestinal microsomes. Gefitinib inhibited the formation of NPC in liver and small intestinal microsomes.

引用

页码：1785 / 1790

页数：6

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