A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein (CETP). [1][2][3][4] They are intended to reduce the risk of atherosclerosis (a cardiovascular disease) by improving blood lipid levels. At least three medications within this class have failed to demonstrate a beneficial effect. [5]

Four CETP inhibitors have substantially increased HDL-C levels in dyslipidemic patients. This review will discuss the current status and future prospects of CETP inhibitors in the treatment of CHD. At present anacetrapib by Merck and evacetrapib by Eli Lilly are under development.

Small molecule inhibitors of CETP have also been developed and four of them have been studied in large scale cardiovascular clinical outcome trials. This review describes the structure of CETP and its mechanism of action.

2017年10月10日 · Treatment with CETP inhibitors, either alone or in combination with statins, could provide another option for patients with coronary disease who require further reduction in LDL (low-density lipoprotein) and non-HDL-C.

The development of CETP inhibitors was motivated by the discovery that humans with genetic CETP deficiency have markedly elevated levels of HDL cholesterol (HDL-C), as well as reduced levels of LDL cholesterol (LDL-C), a profile that is typically associated with reduced atherosclerosis. 1 CETP inhibitors were subsequently shown to raise HDL-C ...

In summary, of the four CETP inhibitors that have been brought to clinical trials, three have been abandoned due to lack of clinical benefit or off-target effects. Anacetrapib and TA-8995 remain in development.

2021年11月26日 · Anacetrapib was the first CETP inhibitor to be proven effective in reducing ASCVD risk. In addition, CETP inhibitors have been shown to lower the risk of new-onset diabetes, improve glucose tolerance, and insulin sensitivity.

CETP inhibitors represent a class of drugs aiming to increase HDL-C values through the inhibition of the heteroexchange of neutral lipids (triglycerides and cholesterol esters) between HDL particles and triglyceride-rich lipoproteins. From: Diabetes Research and Clinical Practice, 2018

A CETP inhibitor is a type of medication that blocks the activity of the plasma glycoprotein CETP, leading to an increase in high-density lipoprotein cholesterol levels without providing significant clinical cardiovascular benefits.

Development of cholesteryl ester transfer protein (CETP) inhibitors for coronary heart disease (CHD) has yet to deliver licensed medicines. To distinguish compound from drug target failure, we compared evidence from clinical trials and drug target ...