Cholesterol absorption as a target for the treatment of hypercholesterolemia

: Hypercholesterolemia is a major risk factor for atherosclerosis. HMG-CoA Reductase inhibitors (statins), which block hepatic synthesis of cholesterol, are the mainstay of therapy of hypercholesterolemia. Recent trials have demonstrated the importance of maintaining very low LDL-cholesterol levels in high-risk patients. Such low levels are sometimes hard to reach with statin monotherapy. Another source of cholesterol is intestinal absorption of dietary cholesterol and bile salts. Recent studies have elucidated the mechanism of intestinal cholesterol absorption. Ezetimibe, a specific inhibitor of cholesterol absorption can be used as an add-on therapy to statins in order to achieve treatment goals.