Cytochrome P450 Induction and Inhibition Assays

Human CYP450 enzymes play an important role in the drug metabolism. Even subtle changes in the activities of CYP enzymes may cause severe drug-drug interactions. The aim of Creative Bioarray is to help our clients with evaluating the interaction potential of your compounds.

Cytochrome P450 (CYP) enzymes dominates the clearance of xenobiotics. Three families of P450 enzymes (CYP1, CYP2, and CYP3) are all involved in the metabolic process, and CYP1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4, 3A5 are responsible for the metabolism of the majority of drugs. There are approximately 75% of the total metabolic enzymes are of the CYP450 family. To address this issue, comprehensive CYP inhibiting or inducing properties should be assessment in the early developing stage of candidate compounds.

For CYP Induction assay, induction of CYPs may cause increased side-effects of DDI, including low recurrence rate due to decreased plasma concentration, or secondary metabolite toxicity. In order to sufficiently evaluate the property, Creative Bioarray offers professional CYP induction test service in accordance with FDA and EMA’s guidelines.

Cytochrome P450 induction assay protocol

Test platformFresh or freeze preserved human hepatocytes
CYP isoformsCYP1A2, CYP2B6, and CYP3A4
Drug Concentration0, 0.25, 0.5, 1, 2, 5,10, 25 μM
(different concentrations available)
Measurement MethodEnzymatic activity: fluorescent or LC-MS/MS
quantification.
mRNA levels: qRT-PCR.
Controls (Negative and positive)Different isoform specific inhibitors to minimize
false results.
Turnaround Time2-3 Days
DataReport, mRNA levels, concentration of
metabolite of probe substrate, Emax, EC50.

In addition to CYP induction, CYP Inhibition assay is also an essential part of DDI assessment in the early developing stage of new compounds.

Cytochrome P450 inhibition assay protocol

Test platformFresh or freeze preserved human hepatocytes
CYP isoformsCYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19,
CYP2D6 and CYP3A4
Measurement MethodLC-MS/MS
ControlsDifferent isoform specific inhibitors to minimize false
results
Turnaround Time2-3 Days
DataIC50, Standard error of IC50

Creative Bioarray provides considerable testing services with high-quality data and detailed assay services, to help clients fully understand CYP-related properties. For more information about our services, please feel free to contact us.

For research use only. Not for any other purpose.