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 ENZYME INHIBITION

Enzyme Inhibition

The primary purpose of evaluating drugs as inhibitors of CYP enzymes in vitro is to determine their perpetrator or precipitant potential before advancing a drug candidate to a late stage of development. XenoTech offers well-designed, in vitro studies that meet or exceed FDA's latest guidance.  

XenoTech’s study design evaluates drug candidates as both direct-acting and time-dependent inhibitors of CYP enzymes in human liver microsomes. Our study design allows us to screen for inhibition by metabolites and features low protein concentration and short incubation times to minimize artifacts caused by protein binding, metabolic instability of the test article and excessive metabolism of the marker substrate. We offer various options for follow up studies to support the further characterization of those drug candidates that are identified as potent direct-acting inhibitors or time-dependent inhibitors. 


STUDY DETAILS


ASSAY SELECTION
TEST SYSTEM
INCUBATION CONDITIONS
INHIBITORS
AUTOMATION AND ANALYSIS
RESULTS
FOLLOWUP STUDIES
ENZYME INHIBITION DECISION TREE 


RELATED INFORMATION


FDA’S latest guidance document (PDF)
XenoTech Products: Human Liver Microsomes