Ezetimibe (Zetia) is a novel, selective cholesterol absorption inhibitor. Ezetimibe blocks the absorption of dietary and biliary cholesterol within the brush-border enzyme system of the small intestine. Ezetimibe does not appear to alter or decrease the absorption of bile acids, fatty acids, fat-soluble vitamins, or triglycerides. It is labeled for use in the treatment of primary hypercholesterolemia, either as monotherapy or in combination with statins. It also is labeled for the treatment of homozygous familial hypercholesterolemia in conjunction with statins and as adjunctive therapy to diet in the treatment of homozygous sitosterolemia (a rare, inherited, plant sterol storage disease).