Physiochemical drug properties associated with in vivo toxicological outcomes

Physiochemical drug properties associated with in vivo toxicological outcomes
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DOI:
10.1016/j.bmcl.2008.07.071
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发表时间:
2008-09-01
影响因子:
2.7
通讯作者:
Zhang, Yao
Zhang, Yao
中科院分区:
医学4区
文献类型:
--
作者:
Hughes, Jason D.;Blagg, Julian;Zhang, Yao

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从245种临床前辉瑞化合物的动物体内耐受性(IVT)研究数据集推断药物理化性质与毒性之间的关系;发现极性较低、亲脂性较高的化合物发生毒性事件的可能性增加。这一趋势在广泛的毒性类型和广泛的化学空间中都存在。(C)2008爱思唯尔有限公司保留所有权利。
Relationships between physicochemical drug properties and toxicity were inferred from a data set consisting of animal in vivo toleration (IVT) studies on 245 preclinical Pfizer compounds; an increased likelihood of toxic events was found for less polar, more lipophilic compounds. This trend held across a wide range of types of toxicity and across a broad swath of chemical space. (C) 2008 Elsevier Ltd. All rights reserved.