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Ezetimibe therapy: mechanism of action and clinical update

Authors Phan BAP, Dayspring TD, Toth PP

Received 7 May 2012

Accepted for publication 23 May 2012

Published 3 July 2012 Volume 2012:8 Pages 415—427


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Binh An P Phan,1 Thomas D Dayspring,2 Peter P Toth3

1Division of Cardiology, Loyola University Medical Center, Maywood, IL, USA; 2Foundation for Health Improvement and Technology, Wayne, NJ, USA; 3CGH Medical Center, Sterling, IL, USA

Abstract: The lowering of low-density lipoprotein cholesterol (LDL-C) is the primary target of therapy in the primary and secondary prevention of cardiovascular events. Although statin therapy is the mainstay for LDL-C lowering, a significant percentage of patients prescribed these agents either do not achieve targets with statin therapy alone or have partial or complete intolerance to them. For such patients, the use of adjuvant therapy capable of providing incremental LDL-C reduction is advised. One such agent is ezetimibe, a cholesterol absorption inhibitor that targets uptake at the jejunal enterocyte brush border. Its primary target of action is the cholesterol transport protein Nieman Pick C1 like 1 protein. Ezetimibe is an effective LDL-C lowering agent and is safe and well tolerated. In response to significant controversy surrounding the use and therapeutic effectiveness of this drug, we provide an update on the biochemical mechanism of action for ezetimibe, its safety and efficacy, as well as the results of recent randomized studies that support its use in a variety of clinical scenarios.

Keywords: bile, coronary artery disease, ezetimibe, low-density lipoprotein cholesterol, Nieman pick C1 like 1 protein, statin

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