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Inhibition of Acyl-CoA Cholesterol Acyltransferase by F12511 (Eflucimibe): Could it be a New Antiatherosclerotic Therapeutic?
Article first published online: 28 JUN 2008
DOI: 10.1111/j.1527-3466.2007.00030.x
2008 The Authors. Journal Compilation © 2008 Blackwell Publishing Ltd
Additional Information
How to Cite
López-Farré, A. J., Sacristán, D., Zamorano-León, J. J., San-Martín, N. and Macaya, C. (2008), Inhibition of Acyl-CoA Cholesterol Acyltransferase by F12511 (Eflucimibe): Could it be a New Antiatherosclerotic Therapeutic?. Cardiovascular Drug Reviews, 26: 65–74. doi: 10.1111/j.1527-3466.2007.00030.x
Publication History
- Issue published online: 28 JUN 2008
- Article first published online: 28 JUN 2008
- Abstract
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Keywords:
- ACAT inhibitors;
- Atherosclerosis;
- Cholesteryl esters;
- Eflucimibe
Lipid-lowering strategies, particularly with statins, have been extremely useful in the prevention of cardiovascular disease. However, many patients who receive statin monotherapy do not achieve the desired cardiovascular benefits. Accumulation of cholesteryl esters within macrophages constitutes the hallmark of foam cells during atherogenesis. The action of acyl-coenzyme A (CoA): cholesterol acyltransferase (ACAT) leads to formation of cholesterol esters. There are two different ACAT isoforms: ACAT1 and ACAT2. A considerable interest to develop ACAT inhibitors has been emerging. This review has been focused on the current knowledge about a new ACAT inhibitor, F12511 or eflucimibe, and more particularly on its antiatherosclerotic properties.