Reaction: Ezetimibe to 1 product

Reaction
Reaction type
glucuronidation
Direction
Major circulating metabolite?
Yes
Spontaneous?
No
Activity
active
References
  1. 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
EnzymeKmVmaxRole
UDP-glucuronosyltransferase 1-1Not AvailableNot Availableconfirmed
UDP-glucuronosyltransferase 1-3Not AvailableNot Availableconfirmed
UDP-glucuronosyltransferase 2B15Not AvailableNot Availableconfirmed