Cholesteryl Ester Transfer Protein Inhibitors: Trials and Tribulations

The cholesteryl ester transfer protein (CETP) is a plasma protein that plays an important role in the transfer of lipids between plasma lipoproteins. The CETP inhibitors have been widely studied as a pharmacologic therapy to target plasma cholesterol in order to reduce the risk of atherosclerotic ca...

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Bibliographic Details
Published in:Journal of cardiovascular pharmacology and therapeutics 2017-03, Vol.22 (2), p.99-104
Main Authors: McLain, Julian Hardy, Alsterda, Andrew Jacob, Arora, Rohit R.
Format: Article
Language:English
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Summary:The cholesteryl ester transfer protein (CETP) is a plasma protein that plays an important role in the transfer of lipids between plasma lipoproteins. The CETP inhibitors have been widely studied as a pharmacologic therapy to target plasma cholesterol in order to reduce the risk of atherosclerotic cardiovascular disease . Using CETP inhibitors as cholesterol modifiers was based on the genetic research that found correlations between CETP activity and cholesterol levels. Although CETP inhibitors are successful at altering targeted cholesterol markers, recent phase 3 outcome trials have shown limited benefit on cardiovascular outcomes when combined with the current standard of care. We discuss the science of CETP inhibition, compare the CETP inhibitors developed (torcetrapib, evacetrapib, dalcetrapib, and anacetrapib), the findings from the CETP inhibitor trials, and the future outlook for CETP inhibitors in cholesterol modification.
ISSN:1074-2484
1940-4034
DOI:10.1177/1074248416662349