CETP inhibitor
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. This category of drugs substantially increases HDL and reverse cholesterol transport. As of 2015, these drugs have generally failed in clinical trials, either causing a marked increase in deaths (torcetrapib), or having no meaningful clinical improvement despite HDL increases (dalcetrapib, evacetrapib).
In testing:
- Anacetrapib, encouraging phase IIb interim results in 2010. Two phase III trials are running until 2017.
- TA-8995, Phase II results reported in 2015.[5]
Failed:
- Torcetrapib, failed in 2006 - excess deaths in phase III.
- Dalcetrapib, development halted in May 2012 when Phase III trials failed to show clinically meaningful efficacy. [6]
- Evacetrapib, development discontinued in 2015 due to insufficient efficacy[7]
Mechanism
CETP inhibitors inhibit cholesterylester transfer protein (CETP), which normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL). Inhibition of this process results in higher HDL levels (the "good" cholesterol-containing particle) and reduces LDL levels (the "bad" cholesterol).[citation needed]
References
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