Phase I and II Metabolism Services

Eurofins Pharma Discovery Services offers an industry-leading portfolio of in vitro services, including Phase I and Phase II enzyme assays, designed to help you understand the metabolic profile of your compound.
 
The Phase I (e.g. cytochrome P450’s) and Phase II (e.g. GSTs and UGTs) metabolizing enzymes in the liver are responsible for the majority of drug metabolism occurring in the body. Drugs can also interact with these enzymes, by inhibiting their enzymatic activity (CYP inhibition) or through activation of nuclear receptors leading to induction of their gene expression (CYP induction).
 
Metabolism-mediated drug-drug interactions (DDI) can occur when a drug affects the Absorption, Distribution, Metabolism, Excretion (ADME), and Pharmacokinetics (PK) of simultaneously administered drugs by altering the activities of drug metabolizing enzymes and/or drug transporters.
 
Following regulatory guidelines set forth in the FDA and EMA Guidance document (2012)1, we provide CYP inhibition and induction assays for 3A4, 2B6, 2D6, 1A2, 2C8, 2C9, 2C19 and other isoforms. Our CYP induction assays can performed by measuring gene expression levels by real time qPCR (mRNA analysis) or by traditional methods of measuring enzyme activity and are available in cultured primary hepatocytes from human and animal species. All of our CYP assays can be ordered individually, combined, or as a selection of key stability services provided in our drug candidate assessment packages to provide cost savings.