New azetidinone cholesterol absorption inhibitors

Author: Bai Xu  

Publisher: Informa Healthcare

ISSN: 1354-3776

Source: Expert Opinion on Therapeutic Patents, Vol.17, Iss.7, 2007-07, pp. : 791-797

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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.