Discovery Plus™ Screening: Cytochrome P450 (CYP) Enzyme Induction
Our Cytochrome P450 (CYP) Enzyme Induction Screening service gives you quick, low-cost induction data for one or more compounds to inform you of your drug candidates’ potential to upregulate major cytochrome P450 (CYP) drug-metabolizing enzymes within 15 days, allowing preliminary ADME / PK evaluation and efficient prediction of drug-drug interactions (DDI) in early stages of drug development.
Discovery Plus™ CYP Induction is more than just a screening service. Our 96-well plate format allows up to 10 different compounds to be tested at 3 concentrations and positive controls in triplicate wells. Discovery Plus™ Induction is a non-GLP service that provides customers with CYP3A4 mRNA fold change data more quickly, saving time and money; get data from a Discovery Plus™ CYP enzyme induction screening study sooner to make risk-based decisions and get you through the pipeline more efficiently.
This service is best utilized for compounds that are in the discovery or early development phase. For compounds that will be submitted for regulatory agency approval, please see our definitive CYP Induction service.
Our Approach to Medium-Throughput Induction Screening
Our Discovery Plus™ design offers the most value in the industry, providing you important data quickly, at a very attractive price point.
Our specialized medium-throughput assay design allows you to quickly evaluate your drug candidate’s effect on CYP3A4 fold change in mRNA. This service yields data presented in a tabular summary of fold change, compared to the vehicle for CYP3A4 (other CYPs are available).
Pre-characterized cryopreserved primary hepatocytes are treated in a 96-well plate format for ~24 hours with the vehicle, test article at 3 concentrations, and positive control(s) in triplicate wells. The expression levels of mRNA are determined utilizing real-time quantitative reverse transcription-polymerase chain reaction (qRT-PCR) technology by the cDNA ddCt method (samples normalized to endogenous housekeeping gene). The fold induction is then calculated as test compound over the vehicle control.
Cytochrome P450 Enzyme mRNA Fold Induction and Screening Study Design
- Measures mRNA fold induction in CYP3A4 (other CYPs may be substituted)
- Utilizes qRT-PCR techniques for mRNA measurement
- Design allows up to 10 NCEs at 3 concentrations and positive controls, performed in triplicate
- Data presented in tabular summary of fold induction
- Offered as a non-GLP service