|Reaction phenotyping assays have become an integral part of drug discovery screening as tools to minimize drug–drug interaction potential and to avoid complications due to polymorphic expression of drug metabolizing enzymes.
In vitro reaction phenotyping methods enable a prediction of human pharmacokinetics and dosages and determine the significance of individual human-specific drug metabolizing enzymes.
Reaction phenotyping is very useful to predict the in vivo metabolic clearance and the contribution of individual drug metabolizing enzymes to the total in vivo clearance. A drug with a metabolic clearance (e.g. >40% of the total clearance) and metabolized by a polymorphic enzyme and/or a primary enzyme (e.g. >30-50% of the total metabolic clearance) has an increased risk of drug-drug interactions and/or individual variation.
At Quintara Discovery, we have validated assays for reaction phenotyping. The studies can be conducted in the following ways: