Quintara Discovery

CYP450 Induction

CYP450 induction-mediated drug-drug interaction is a major concern in clinical practice.CYP induction can be associated with either a reduction in the therapeutic efficacy of co-medications or an induction in reactive metabolite-induced toxicity.

Because CYP induction is a metabolic liability in drug therapy, it is highly desirable to develop new drug candidates that are not potent CYP inducer to avoid the potential of CYP induction-mediated drug interactions.

Assay Methodology

Quintara Discovery can conduct CYP450 induction assays for CYP1A2, CYP2B6 or CYP3A4 in human hepatocytes by evaluating their catalytic activities and mRNA expression levels. The assay is performed by incubating the test compounds with human hepatocytes (platable cryopreserved or fresh) for 4 days, followed by measurement of the activity measurement using specific probe substrates and the mRNA levels by qPCR.