About Ezetimibe Cholesterol Absorption Inhibitor, 2-Azetidinone derivative, Hypolipidemic agent. Mechanism of Action of Ezetimibe It reduces the absorption of cholesterol from the intestine by localising at the brush border of the small intestine, where it inhibits the absorption of cholesterol from the diet. Specifically, it appears to bind to the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelium, a critical mediator of cholesterol absorption. This decreased cholesterol absorption leads to an increase in LDL-cholesterol uptake into cells, thus decreasing levels in the blood plasma. Indications for Ezetimibe 1. Adjunct to dietary measures and statin in primary and homozygous familial hypercholesterolaemia 2. Adjunct to dietary measures in homozygous familial sitosterolaemia