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Identification of drug metabolizing enzymes with admescope

5 April 2013

Identifying the enzyme/s responsible for the metabolism of the new chemical entity (NCE) is increasingly important in drug discovery process. This information enables the prediction of the potential drug-drug interactions with co-medicated drugs as well as estimation of inter-individual differences in the metabolism of the drug.

cypIDscreen is cost-effective early phase screen assay for nine most important CYP enzymes involved in drug metabolism; CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. The assay is conducted with recombinant human CYP enzymes and the formation of metabolites is be analyzed with UPLC/Q-TOF-MS, thus delivering information of enzymes involved with formation of each metabolite separately. Also other isoforms can be included upon request.

cypIDprofile provides more comprehensive evaluation of metabolizing CYP enzymes utilizing two independent methods for elucidation according to FDA recommendations. In addition of using recombinant human CYP enzymes as above, the metabolite formation will be also monitored in human liver microsomes with CYP-specific inhibitors using optimal kinetic conditions.

UGTscreen utilizes human recombinant UGT enzymes 1A1, 1A3, 1A4, 1A6, 1A9, 2B7 and 2B15 for elucidation of enzymes behind formation of glucuronide conjugates. Also other isoforms can be included upon request. Formation of conjugates is monitored UPLC/Q-TOF-MS analysis.

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