CETP inhibitor


A CETP inhibitor is a member of a class of drugs that inhibit cholesterylester transfer protein. They are intended to reduce the risk of atherosclerosis by improving blood lipid levels. At least three medications within this class have failed to result in benefits however.

Types

These drugs have generally failed in clinical trials, either causing a marked increase in deaths, or having no meaningful clinical improvement despite HDL increases.
Failed:
Succeeded:
Drugs in this class substantially increase HDL, lower LDL, and enhance reverse cholesterol transport.
CETP inhibitors inhibit cholesterylester transfer protein, which normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins. 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.

Pharmacogenomics

In 2015, a pharmacogenomic sub-study of the dal-OUTCOMES clinical trial on 5,749 individuals identified a genetic variant in the ADCY9 gene which modulates response to dalcetrapib. In patients with the rs1967309 'AA' genotype, there was a significant reduction in the rate of cardiovascular events in the dalcetrapib arm whereas non-carriers were at increased risk. The efficacy of dalcetrapib in the genetic sub-population is currently being investigated in the dal-GenE trial.

Chemical structures