4.5 Article

Physiochemical drug properties associated with in vivo toxicological outcomes

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 17, Pages 4872-4875

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.07.071

Keywords

toxicity; polar surface area; ClogP; adverse events

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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.

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