Gene expression data from primary human hepatocytes treated with idelalisib for 24 h

Idelalisib is a phosphatidylinositol 3-delta kinase inhibitor that has shown good efficacy in treating some hematologic malignancies. Rare, but potentially serious liver toxicity was associated with idelalisib use in clinical trials. The objective of this study was to evaluate the idelalisib-induced activation of stress response pathways in human hepatocytes to inform mechanisms of liver injury observed in the clinic Primary human hepatocytes from three donors were sandwich cultured and assayed for global gene expression across 5 concentrations of idelalisib after a 24 h exposure. The most significantly enriched pathway among genes upregulated in response to idelalisib was “Endoplasmic Reticulum Stress”. These data suggest that oxidative stress is a dominant mechanism contributing to liver injury associated with idelalisib. 24 samples were analyzed representing N=1 per donor and treatment