The main metabolic site of the drug is the liver. Liver-derived systems, such as liver slices, subcellular liver fractions, and intact hepatocytes are typically used to assess the metabolism of new chemical entities (NCEs). Hepatocytes, having an intact cell membrane and physiological concentrations of phase I and phase II enzymes in addition to cofactors, are generally considered to be the most accurate model for predicting whole liver drug clearance. NCEs can be screened and prioritized based on estimates of metabolic half-life or intrinsic clearance values obtained from metabolic stability studies. Moreover, hepatocyte metabolic screening assays allow drug developers to focus on the improvement of compounds through structural-activity relationships and prevent the progression of labile compounds to more costly in vivo research.
Creative Bioarray's hepatocyte stability assay monitors the disappearance of substrates in the presence and absence of hepatocytes. This assay can determine the fate of the drug in the body and calculate its clearance rate. Using hepatocytes from a variety of species, we can help determine the species-specificity of hepatic clearance and translate animal data to the human scenario.
Test compound concentration
0, 5, 15, 30, 45, 60, 90, 120 minutes
Positive control: Testosterone, Ethoxycoumarin, or Midazolam
Negative control with vehicle
Number of replicates
Intrinsic clearance (CLint)
%Disappearance of parent compound
200 µL 10 mM stock in DMSO
Human, monkey, minipig, dog, rabbit, rat, mouse