Cytochrome P450 (CYP) enzymes play a major role in the metabolism of the majority of xenobiotics; therefore, a change in their activities, either by inhibition or induction, may have severe effects on the pharmacokinetics and pharmacodynamics of drugs. For example, inhibition of CYP enzyme(s) responsible for metabolism of a co-administered drug may delay its excretion and raise its plasma concentration to toxic levels.
Cells that perform reliably in inhibition assays should have reproducible Phase I and II enzyme activities at levels that allow for a good dynamic range for inhibition. upcyte® Hepatocytes have donor-dependent - but sufficient - basal enzyme activities and, as such, they represent a reliable tool for drug inhibition studies. To help you establish the upcyte® Hepatocytes in your drug inhibition studies, upcyte technologies developed an upcyte® Hepatocyte CYP inhibition protocol.