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CYP identification, inhibition and induction
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The cytochrome P450 enzymes, CYPs, are involved in the Phase I drug metabolism and bioactivitation, by oxidizing their ligands. During ADME studies, the oxidizing CYP enzyme is identified, the compounds ability to inhibit the CYP is studied as well as the ability to induce the activity of the CYP enzyme. CYP inhibition of induction are a major source of adverse drug effects, affecting the metabolism and clearance of other molecules, which are ligands for the same CYP enzyme.
We provide our customers with a comprehensive set of CYP enzyme - drug interaction studies. These include
The methods we use for the studies of CYP enzymes responsible for oxidative metabolism include
InhibCYPCost-effective study to unravel the inhibition potential of NCE towards CYP enzymes. Utilizes cocktail incubation of CYP specific probe compounds. Evaluation of potential drug-drug interactions. Used for lead molecule selection and drug candidate characterization. CYPidThis study pinpoints those CYP enzymes contributing to the production of the metabolites of NCE. Indirect method that utilizes the use of CYP selective inhibitors. Evaluation of potential drug-drug interactions. Used for lead molecule selection and drug candidate characterisation. The various alternatives for CYP identification are provided below reCYPidAs above, to pinpoint metabolizing CYP enzymes, but now the method is direct and utilizes recombinant CYP enzymes. Evaluation of potential drug-drug interactions. Used for lead molecule selection and drug candidate characterisation. CYPid and reCYPid are complementary: both studies should point to the same direction to be able to reliably state that a certain CYP enzyme produces a certain metabolite. Metabolite profile of NCE should be known before the studies can be performed. CYP activityWe also provide analysis of the activities of different CYP enzymes. This analytics based on a luminescent method to measure CYP activity. This analytics is based on P450-Glo™ system, where the assays are derivatives of beetle luciferin. The derivatives are not substrates for luciferase but are converted by cytochrome P450s to luciferin, which in turn reacts with luciferase to produce light. The amount of light produced is directly proportional to the activity of the cytochrome P450. The luminescence based CYP activity Mechanism based inhibitionMechanism based inhibition analysis the potential inhibition caused by the compound on the known activity of CYPs on a cocktail of known small molecules. MetaboEnzymeThis study identifies the involvement of many other than CYP enzymes activities on the compound. This is based on using recombinant enzymes from UGT, SULT, AldO, GE, GST, FMA and MAO families All our services are tailored to the customers need. Click here for our other ADME/DMPK services. |
Please follow this link to retrieve a detailed fact sheet of the InhibCYP service