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

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 cytotoxicit...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 20; no. 17; pp. 5308 - 5312
Main Authors Greene, Nigel, Aleo, Michael D., Louise-May, Shirley, Price, David A., Will, Yvonne
Format Journal Article
LanguageEnglish
Published Amsterdam Elsevier Ltd 01.09.2010
Elsevier
Subjects
Animals
Attrition
Biological and medical sciences
c log P
Cytotoxicity
In Vitro Techniques
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
Physico chemistry
Rodentia
Toxicity Tests
Toxicology
TPSA
Cytotoxicity
Toxicology
Physico chemistry
TPSA
Attrition
c log P
Human
Drug
Toxicity
Liver
Prediction
Partition coefficient
In vitro
Research and development
In vivo
Classification
Epithelial cell
Safety
Lipophilicity
Physicochemical properties
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.06.129