Cytochrome P450 enzymes are members of one of the most relevant families of drug metabolizing enzymes. Alterations in their expression levels can affect the clearance of drugs and lead to potential drug–drug interactions (DDI). CYP induction can be mediated by various mechanisms, including activation of nuclear receptors, such as the pregnane X receptor (PXR), aryl hydrocarbon receptor (AhR), or constitutive androstane receptor (CAR).
Our CYP induction assay is optimized to detect the induction of CYP1A2, CYP2B6, and CYP3A4 on mRNA expression, as well as on enzyme activity level, as a surrogate for the activation of PXR, AhR, and CAR. HepaRG cells are incubated in the presence of different test compound concentrations, and the effect on gene expression is determined by qRT-PCR. The change in activity is determined in parallel by LC-MS/MS analysis of metabolite formation from CYP-isoform-specific reactions. Aiming at providing the highest quality of data, our assay provides additional information on cell viability using microscopy as well as biochemical cytotoxicity measurements.
By using our CYP induction assay, your drug discovery project benefits from an early understanding of your compounds’ potential to interact with other drugs and identification of any potential safety concerns. Our experienced scientists are there to consult with you on your specific questions and support you in the choice, evaluation, and interpretation of the results.