CYP Induction
| CYP450 induction-mediated drug-drug interaction is a major concern in clinical practice. CYP induction can result in either a reduction in the therapeutic efficacy of co-medications or an increase in toxicity due to elevated levels of metabolites.
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 MethodologyQuintara Discovery conducts CYP450 induction assays for CYP1A2, CYP2B6 or CYP3A4 in platable human hepatocytes by evaluating their mRNA expression levels and/or catalytic activities as compared to vehicle control and FDA-recommended inducers. The assay is performed by incubating the test compounds and controls with human hepatocytes (platable cryopreserved or fresh) for 3-4 days, followed by measurement of mRNA levels by qPCR and/or functional activity tests using specific probe substrates. |
||