Reaction: Ezetimibe to 1 product

glucuronidationMajor circulating metaboliteMetabolism of Ezetimibe

Ezetimibe is converted to Ezetimibe glucuronide by UDP-glucuronosyltransferase 1A1, UDP-glucuronosyltransferase 1A3, and UDP-glucuronosyltransferase 2B15.

Direction
Activity
active
Comments
The 4-hydroxyphenyl group of ezetimibe is glucuronidated. Ezetimibe-glucuronide accounts for the majority (80–90%) of total ezetimibe concentrations measured in human plasma, and it is reported to retain some pharmacological activity in inhibiting intestinal cholesterol absorption with less potency compared to the parent compound.

What you can answer from here — as of June 11, 2018

3EnzymesEach linked to its target card
Listed above
1ReferenceThe literature this reaction is curated from
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Which other drugs are metabolised by UDP-glucuronosyltransferase 1A1, UDP-glucuronosyltransferase 1A3, and UDP-glucuronosyltransferase 2B15, and which of those pairings are clinically significant?

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