CYP Inhibition Assays

Eurofins Discovery provides a valuable tool to explore potential drug interactions of your compounds in the early discovery phase: our Cytochrome P450 (CYP) platform. Our platform will help you evaluate if your compounds inhibit the activity of CYP isozymes and further understand and optimize them on the strength of our skilled chemistry capabilities.
 
Exploration is important since CYP is in the hemoprotein family, which plays a vital role in drug metabolism. CYP catalyzes most Phase I oxidative reactions in the liver introducing polar groups into xenobiotics. CYP metabolizes over 90% of clinical drugs and detoxifies poisonous compounds. Changes in CYP’s activity may affect the metabolism and clearance of drugs. In addition to catabolism, CYP also interacts with drugs that either induce the synthesis of CYP or inhibit the activity of CYP. Within this context, CYP P450 assays are widely used in the early phases of the drug discovery workflow and in the ADME evaluation of candidate molecules.
 
Drugs that inhibit a CYP isozyme may cause a concentration increase of other drugs metabolized by the same isozyme (drug-drug interaction studies), and result in drug toxicity. In the same way, drugs that induce a CYP isozyme may reduce concentrations of drugs metabolized by the same isozyme, and lead to sub-therapeutic concentration and treatment failure.
 
Our CYP Services determine the inhibition of the major CYP enzymes using fluorescent technology (fluorescent substrates plus recombinant human CYP enzymes). Be confident that when it comes to ADME applications, Eurofins Discovery’s assays are in accordance to international regulatory guidelines set by the regulatory agencies (including the U.S. FDA and European EMA), and include CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4.