CYP Induction

CYP Induction

Predict the potential drug-drug interactions of your test compound or xenobiotic using our Cytochrome P450 (CYP) Induction assay.   

In the human body, Cytochrome P450 (CYP) enzymes play a major role in the metabolism of drugs and chemicals and therefore, CYPs are of primary interest in the assessment of drug-drug interactions.  Induction of CYPs can lead to reduced efficacy and half-life or an increase in toxicity.  When one drug induces the CYPs responsible for the metabolism of another drug, a drug-drug interaction can occur.  Therefore, it is crucial to assess the CYP induction potential of a test compound.  Our CYP Induction assays assess mRNA induction and/or catalytic activities of CYP1A2, CYP2B6 and CYP3A4 in fresh human primary hepatocytes in accordance with the FDA guidelines on Drug Interaction Studies.1

CYP Induction assay overview

Cultured primary hepatocytes from three donors are exposed to the controls and the test compound for 72 hours.  The test compound should be assessed at several concentrations surrounding the expected human plasma drug concentrations.  After the exposure, the mRNA is isolated and CYP1A2, CYP2B6 and CYP3A4 gene expression levels are analyzed by real time RT-PCR (qRT-PCR).  The data are normalized to housekeeping genes and presented as fold induction vs negative (vehicle) control. IONTOX can also evaluate changes in CYP activity toward specific substrates.  This information provides an added level of confidence.

CYP Induction example output

IONTOX’s CYP induction study can be combined with our Human Dynamic Multiple Organ Plate to assess the effects of the tested compound or metabolites on subsequent tissues, such as the kidney or lung.