Comparative Metabolism of Eight Model Pharmaceutical Compounds in Rat- and Human- Liver Microsomes, Suspension Hepatocytes, and Micropatterned Co-cultures of Primary Hepatocytes

In vitro metabolism evaluations for compounds in early development are typically conducted using liver microsomes and suspension hepatocytes. While these systems have been serving the drug development community, they have their limitations, with examples of “metabolite surprises” where metabolites which were not predicted or observed in vitro or in vivo during pre-clinical studies, were observed in the clinic. Such surprises can have a significant impact on the timeline of a drug development program and has prompted investigations aimed at developing in vitro systems that can more accurately predict human in vivo metabolism.