Ezetimibe belongs to a new class of lipid-lowering agents that selectively inhibit the intestinal absorption of cholesterol and related plant sterols. The molecular target of ezetimibe is the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is responsible for the intestinal uptake of cholesterol and phytosterols. Its action is localized at the brush border of the small intestine where it inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. Ezetimibe and statins, which are the most important part of the antihyperlipidemic therapy, have complementary mechanisms of action. It have been recently demonstrated that administration of ezetimibe with a statin not only lowers LDL cholesterol level, but is also effective in reducing the risk of heart attack and stroke.