ezetimibe + ursodiol

Ezetimibe + ursodiol is a combination of two small molecule drugs used experimentally to promote cholesterol elimination. Ezetimibe is a cholesterol absorption inhibitor that acts at the brush border of the small intestine by selectively blocking the Niemann-Pick C1-Like 1 protein (NPC1L1), thereby reducing intestinal cholesterol uptake and lowering plasma LDL cholesterol. Ursodiol (ursodeoxycholic acid) is a hydrophilic bile acid that increases biliary secretion and reduces hepatic production of cholesterol, as well as dissolving gallstones and treating certain liver diseases. Preclinical studies in mice have shown that this combination can additively increase fecal sterol excretion by both increasing biliary secretion (ursodiol) and reducing intestinal reabsorption (ezetimibe), revealing an alternative pathway for cholesterol elimination independent of ABCG5/ABCG8 transporters[1][5]. In humans, however, clinical trials have not demonstrated increased fecal neutral sterols or reduced LDL-C with this combination compared to monotherapy[6].

Other names

ezetimibe + ursodeoxycholic acidezetimibe + UDCA