Using an in vitro cytotoxicity assay to aid in compound selection for in vivo safety studies

被引：56

作者：

Greene, Nigel ^{[1
]}

Aleo, Michael D. ^{[1
]}

Louise-May, Shirley ^{[1
]}

Price, David A. ^{[1
]}

Will, Yvonne ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 17期

关键词：

c log P; Toxicology; TPSA; Attrition; Cytotoxicity; Physico chemistry; DRUGS;

D O I：

10.1016/j.bmcl.2010.06.129

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Recent publications have demonstrated that using calculated physiochemical properties can help in the design of compounds that have a decreased risk of significant findings in rodent toxicology studies. In this Letter, we extend this concept and incorporate results from a high throughput cytotoxicity assay to help the drug discovery community select compounds for progression into in vivo studies. The results are presented in an easily interpretable odds ratio so that teams can readily compare compounds and progress potential clinical candidates to the necessary rodent in vivo studies. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5308 / 5312

页数：5

共 10 条

[1]

ALEO MD, TOXICOL LET IN PRESS

[2] Drugs, hERG and sudden death [J].