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UGT Inhibition

• Screening using recombinant UGT enzymes
• Analysis with LC/MS/MS to monitor the formation of UGT-specific probe metabolites

Glucuronidation caused by uridine 5'-diphospho-glucuronosyltransferases (UGT) is an important pathway for drug metabolism in humans and other mammals. The inhibition of UGT, although less often observed than CYP inhibition, is a clinically significant form of drug-drug interactions and may lead to toxicity. Therefore, the elucidation of UGT inhibition is recommended by the regulatory authorities especially in cases where direct glucuronidation is one of the major elimation routes for the new chemical entity.

UGT inhibition assays for the isoforms UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7 and UGT2B15 are available using recombinant enzymes with specific substrates and several inhibitor concentrations, delivering IC50 values towards specific UGTs.