In vitro characterization of the human biotransformation and CYP reaction phenotype of ET-743 (Yondelis®, Trabectidin®), a novel marine anti-cancer drug

被引：0
作者：
Esther F. A. Brandon
Rolf W. Sparidans
Kees-Jan Guijt
Sjoerd Löwenthal
Irma Meijerman
Jos H. Beijnen
Jan H. M. Schellens
机构：
[1] Utrecht University,Faculty of Pharmaceutical Sciences
[2] Slotervaart Hospital,Pharmaceutical Sciences
[3] The Netherlands Cancer Institute,Biomedical Analysis—Drug Toxicology
[4] Utrecht University,undefined
来源：
Investigational New Drugs | 2006年 / 24卷
关键词：
ET-743; biotransformation; cytochrome P450 (CYP); conjugation; CYP reaction phenotype;
D O I：
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学科分类号：
摘要：
ET-743 is a potent marine anti-cancer drug and is currently being investigated in phase I and II clinical trials, e.g. in combination with other anti-cancer agents. To assess the biotransformation and CYP reaction phenotype and their potential implications for human pharmacology and toxicology, the in vitro metabolism of ET-743 was characterized using incubations with human liver preparations, cytochrome P450 (CYP) and uridine diphosphoglucuronosyl transferase (UGT) supersomes.
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页码：3 / 14
页数：11
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