Role of UDP-Glucuronosyltransferases in Drug Metabolism and Drug-Drug Interactions
(Date : 5th Oct 2021)
The importance of glucuronidation for
metabolism of xenobiotics in humans is illustrated by the abundance and broad tissue distribution of the enzymes, the diversity of substrates and reactions catalyzed, as well as a number of distinctive UGT enzymes and their genetic polymorphisms. The involvement of UGTs in metabolism of new drug candidates will be presented as it underscores the enzymes’ importance from regulatory and safety perspectives.
Basic biochemical characteristics of UGTs will be reviewed and examples of major forms of glucuronides formed in humans will be presented. Distinctive properties of acyl-glucuronides and their significance for drug-drug interactions will be highlighted.
Factors contributing to underprediction of UGTs’ in vivo contributions to the metabolism of xenobiotics will also be covered. Laboratory approaches aimed at
improving these predictions will be covered, as well.
Key concepts discussed in this webinar will include:
Significance of UGT-mediated metabolism in drug development process
Consequences of formation of acyl-glucuronides
Underprediction of in vivo UGT-mediated metabolism