Ezetimibe therapy: mechanism of action and clinical update

imibe therapy: mechanism of action and clinical update Review (4569) Total Article Views 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: 07 May 2012 Accepted: 23 May 2012 Published: 03 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.