Drug intelligence / Profile preview

ezetimibe + ursodeoxycholic acid

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**EZ-Urso** is an investigational oral co-administration regimen of **ezetimibe** and **ursodeoxycholic acid**. Ezetimibe inhibits the intestinal sterol transporter Niemann-Pick C1-like protein 1, reducing dietary and biliary cholesterol absorption, while ursodeoxycholic acid is a hydrophilic bile acid that alters the bile-acid pool and promotes biliary sterol handling. The regimen was evaluated in a terminated Phase 2 study in nonalcoholic fatty liver disease to test whether the complementary effects could create a net-negative sterol balance, increase fecal cholesterol elimination, and improve liver-function biomarkers. EZ-Urso is not a distinct marketed fixed-dose product; the trial administered separate oral Zetia and Urso Forte products.

Other names
EZ-Urso combination therapyEzetimibe-Ursodiol Combination Therapyezetimibe + ursodiolZetia + Urso Forte
02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)Bile acid pool and biliary cholesterol

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