Abstract
Since their initial discovery, azetidinones have been extensively studied as potent cholesterol absorption inhibitors. Ezetimibe is the first-in-class and only member in the clinics either as a monotherapy or in combination with statins for treatment of hypercholesterolemia. The recent identification of Niemann–Pick C1-like 1 protein in the brush border membrane of the small intestine as a possible molecular target has opened the door for the design and synthesis of new anticholesterol drugs. This article reviews the important literature and patents on cholesterol absorption inhibitors.
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