Ezetimibe therapy: mechanism of action and clinical update.

Article Details

Citation

Phan BA, Dayspring TD, Toth PP

Ezetimibe therapy: mechanism of action and clinical update.

Vasc Health Risk Manag. 2012;8:415-27. doi: 10.2147/VHRM.S33664. Epub 2012 Jul 3.

PubMed ID
22910633 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drugs
Drug Interactions
DrugsInteraction
Ezetimibe
Bezafibrate
The risk or severity of adverse effects can be increased when Bezafibrate is combined with Ezetimibe.