UGT inhibition

The test compound is incubated with human recombinant UGT enzymes (1A1, 1A3, 1A4, 1A6, 1A9, 2B7, 2B15) together with UGT-specific substrates, as single enzyme incubations. The inhibition is observed as reduced level of UGT-specific metabolite formation.
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Test concentrations: 6

Time points: 1

Replicates: 2

Positive controls

UPLC/MS/MS analysis

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% inhibition or IC50 for each UGT

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Full Word/PDF report

Background

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 elimination routes for the new chemical entity.

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