CYP induction screening, PXR activation

Cytochrome P450 (CYP) induction by a new chemical entity results in the increased amount and activity of relevant drug-metabolizing CYPs, which may lead to enhanced metabolism of co-medicated drugs. CYP induction is a relatively slow phenomenon due to gene regulation events, such as nuclear receptor activation and synthesis of mRNA and enzyme. Exposure times for the assays are usually 24 – 72 hours, followed by PXR activation, mRNA and/or CYP activity assessment. As a part of our drug-drug interactions services, the CYP induction screening assays are tailored for cost-efficient simultaneous evaluation of higher number of compounds, whereas the regulatory compliant induction assay with human hepatocytes is a comprehensive package required by FDA and EMA. Each assay delivers CYP induction relative to vehicle control (x-fold) and / or EC50 values if feasible (concentration where 50 % of maximal induction is achieved). The induction assays are available for CYP1A2, CYP2B6 and CYP3A4. Assays for other CYPs are available upon request.