Back to Browse Journals » Vascular Health and Risk Management » Volume 8

Ezetimibe therapy: mechanism of action and clinical update

Authors Phan BAP, Dayspring TD, Toth PP

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

DOI http://dx.doi.org/10.2147/VHRM.S33664

Received 7 May 2012, Accepted 23 May 2012, Published 3 July 2012

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

Download Article [PDF] View Full Text [HTML] 

Creative Commons License This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution - Non Commercial (unported, v3.0) License. The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. Permissions beyond the scope of the License are administered by Dove Medical Press Limited. Information on how to request permission may be found at: http://www.dovepress.com/permissions.php

Readers of this article also read:

Renal interstitial fibrosis induced by high-dose mesoporous silica nanoparticles via the NF-κB signaling pathway

Chen X, Zhouhua W, Jie Z, Xinlu F, Jinqiang L, Yuwen Q, Zhiying H

International Journal of Nanomedicine 2015, 10:1-22

Published Date: 18 December 2014

Proposed criteria for schizophrenia remission

AlAqeel B

Neuropsychiatric Disease and Treatment 2014, 10:619-623

Published Date: 16 April 2014

Dabigatran and myocardial infarction: a foggy scenario

Pontillo D, Patruno N

Vascular Health and Risk Management 2014, 10:45-48

Published Date: 20 January 2014

Corrigendum

Basit A, Riaz M, Fawwad A

Vascular Health and Risk Management 2013, 9:1-2

Published Date: 27 December 2012

Corrigendum

Schneider EW, Johnson MW

Clinical Ophthalmology 2011, 5:1315-1316

Published Date: 16 September 2011

Role of aliskiren in cardio-renal protection and use in hypertensives with multiple risk factors

Eduardo Pimenta, Suzanne Oparil

Vascular Health and Risk Management 2009, 5:453-463

Published Date: 19 May 2009

Prevalence of risk factors, coronary and systemic atherosclerosis in abdominal aortic aneurysm: Comparison with high cardiovascular risk population

Alberto Palazzuoli, Maddalena Gallotta, Giuseppe Guerrieri, Ilaria Quatrini, Beatrice Franci, et al

Vascular Health and Risk Management 2008, 4:877-883

Published Date: 7 September 2008