Bioequivalence and Bioavailability Forum

❝ why only take uncongugated ezetimibe as BE Creteria apart from total ezetimibe any evidence available?

Dear Dr Babu,

Greetings !!

Hope your intented submission is not US as you have to follow OGD while for EU, 90 % BE should be on Ezetimibe (unconjugated) and not on total.

Ezetimibe is primarily metabolized in the small intestine and liver via glucuronide conjugation and produce congugated ezetimibe. (So total includes = Conjugated + Nonconjugated)

As it is a metabolic product, glucoronide formation might be different in individual subjects.

Moreover EU regualtory remains silent about measuring the metabolites.

So you can measure both(eze unconjugated & total), but perform BE only on Unconjugated.