Reaction: Ezetimibe to 1 product
- Reaction
- Reaction type
- glucuronidation
- Direction
- Major circulating metabolite?
- Yes
- Spontaneous?
- No
- Activity
- active
- References
- Kosoglou T, Statkevich P, Johnson-Levonas AO, Paolini JF, Bergman AJ, Alton KB: Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94. [Article]
- 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.
- Enzymes
Enzyme Km Vmax Role UDP-glucuronosyltransferase 1-1 Not Available Not Available confirmed UDP-glucuronosyltransferase 1-3 Not Available Not Available confirmed UDP-glucuronosyltransferase 2B15 Not Available Not Available confirmed