Clinical trials with cholesteryl ester transfer protein inhibitors

Inhibition of cholesteryl ester transfer protein (CETP) has received considerable interest by virtue of its favorable effects on atherogenic and protective lipid parameters. The impact of CETP inhibitors in large clinical outcome trials will be reviewed.

Population and genetic studies demonstrate that low CETP activity associates with lower rates of cardiovascular events. Inhibiting CETP activity in animal models has a favorable impact on experimental atherosclerosis. Although the first CETP inhibitor to advance to an outcome trial proved to have adverse clinical effects and the next agent, a more modest inhibitor, was clinically futile, there continues to be immense interest in the potential to develop nontoxic, potent CETP inhibitors to reduce cardiovascular risk.

The current status of CETP inhibitors in the context of large outcomes trials will be reviewed.