CETP inhibitor

Updated on Sep 23, 2024

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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. 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 clinical trials:

Anacetrapib, encouraging Phase IIb interim results in 2010. Two phase III trials are running until 2017.

Obicetrapib (TA-8995), Phase II results reported in 2015.

Failed:

Torcetrapib, failed in 2006 due to excess deaths in Phase III clinical trials.

Dalcetrapib, development halted in May 2012 when Phase III trials failed to show clinically meaningful efficacy.

Evacetrapib, development discontinued in 2015 due to insufficient efficacy.

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 and reduces LDL levels. CETP inhibitors do not reduce rates of mortality, heart attack, or stroke in patients already taking a statin.

References

CETP inhibitor Wikipedia

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