Hepatocyte‐Based Metabolism, Drug–Drug Interaction, and Toxicity Assays in Drug Discovery and Drug Development to Minimize Attrition

Abstract Primary human hepatocytes are generally considered the “gold standard” forin vitroevaluation of human drug metabolism, drug‐drug interactions (DDIs), and hepatotoxicity. Successful cryopreservation to retain high viability and plateability (ability to be cultured) allows human hepatocytes to be used routinely for experimentation. Assays developed with human hepatocytes include metabolic stability, metabolite profiling, P450 inhibition, P450 induction, andin vitrohepatotoxicity. These assays are routinely used in drug development to minimize metabolic and safety liability of new chemical entities (NCEs).