CETP (Cholesteryl ester transfer protein ) is a plasma protein that facilitates the transport ofcholesteryl esters and triglycerides between the lipoproteins. A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein (CETP). They are intended to reduce the risk of atherosclerosis (a cardiovascular disease) by improving blood lipid levels. Drugs in this class substantially increase HDL ('good cholesterol'), lower LDL ('bad cholesterol'), and reverse the transport of cholesterol.

A Review of Cholesterol Ester Transfer Protein (CETP)

Cholesterol ester transfer protein (CETP) mediates cholesterol ester (CE), phosphorus ester and neutral lipid transfer between lipoproteins, which belongs to the lipid transfer / lipopolysaccharide binding protein family. CETP contains CE and triglyceride binding sites. The degradation of HDL CE was mediated by the decrease of HDL volume and protein content.CETP plays a leading role in reverse cholesterol transport, which is the transport of cholesterol from peripheral tissues to the liver, the increase of cholesterol intake or the increase of it content in endogenous hypercholesterol. Most of CETP in plasma binds to HDL and plays a leading role in reverse cholesterol transport. It is a hydrophobic glycoprotein.

The inhibitor of CETP

is a potent oral selective inhibitor that is currently being developed for the treatment of dyslipidemia. The highest increase in HDL-C in patients with dyslipidemia alone was 129% and the highest decrease in LDL-C was 38%. No effect of Anacetrapib on blood pressure, electrolyte and aldehydes was found in the study.

CETP and disease

Great progress has been made in the study of CETP inhibitors, and the available clinical evidence shows that CETP inhibitors may be an effective and feasible strategy for improving dyslipidemia and preventing and treating cardiovascular diseases. Cholesterol transfer protein regulates lipid metabolism and inhibits lipid metabolism by mediating lipid transport between different lipoproteins. Cholesterol transfer protein has a direct travel effect on regulating concentration. It is expected to further improve the outcome of cardiovascular disease. A number of new inhibitors have been discovered, and more new drugs are expected to enter the clinical research stage in the future.


Fu Jinxiang, Zhu Xiaohui, Gao Beibei, Fu Zhenzhen, Guo Wen, Zhou Hongwen.Effects of estrogen on glucose metabolism and islet function in CETP transgenic mice [J]. Journal of Nanjing Medical University (Natural Science Edition) (08): 1025-1028.

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