CETP inhibitor

Torcetrapib

Anacetrapib

Dalcetrapib

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 by inhibiting reverse cholesterol transport. As of December, 2012, these drugs have generally failed in trials, either causing a marked increase in deaths (Torcetrapib), or having no meaningful clinical improvement despite HDL increases (Dalcetrapib).

In testing:

• Anacetrapib, encouraging phase IIb interim results in 2010. Two phase III trials are running in 2012.
• Evacetrapib, phase II study results published in November 2011 ^[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]

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