Induction and Inhibition assays for UGT enzymes
1 November 2013
We are delighted to announce the release of induction and inhibiton assays for UGT enzymes. UGT enzymes (uridine diphosphate glucuronosyl transferases) are phaseII metabolizing enzymes responsible for biotransformation of many drugs. Recently there has been an increasing interest also in drug-drug interactions involving UGTs and their importance has been highlighted also by regulatory agencies, like EMA and FDA. Evaluation of UGT-interactions is strongly recommended if glucuronidation is a predominant pathway of drug elimination.
UGT inhibition and induction assays are available for UGT1A1, UGT1A9 and UGT2B7 enzymes, and are performed with recombinant enzymes, HepaRG™ cells, or cryopreserved hepatocytes, together with LC/MS/MS analysis of the model reaction metabolites. Inhibition of other UGT-isoforms will be available soon as well.