Preclinical Strategy to Reduce Clinical Hepatotoxicity Using in Vitro Bioactivation Data for >200 Compounds from GSK CRT 2012

Hepatotoxicity

Sakatis, M. Z., et al. Chem. Res. Toxicol., 2012, 25 (10), pp 2067–2082

In this study, 223 marketed drugs (51% associated with clinical hepatotoxicity; 49% non-hepatotoxic) were examined to assess the concordance of in vitro bioactivation data with clinical hepatotoxicity. By using a decision tree developed from the analysis, 45% of the hepatotoxic compounds evaluated were recommended for termination before candidate selection, whereas 10% of the non-hepatotoxic compounds were recommended for termination.

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