The class
Review asks whether anacetrapib and evacetrapib can succeed where torcetrapib and dalcetrapib failed to reduce cardiovascular risk (Annu Rev Med 2014)
Original title: Future of cholesteryl ester transfer protein inhibitors
CETP plays an integral role in plasma lipoprotein metabolism, and despite two clinical failures, CETP inhibitors remained in active development at the time of this review. The authors survey CETP genetics and coronary disease risk, preclinical data linking CETP inhibition to atherosclerosis, and the effects of CETP inhibition on cholesterol efflux and reverse cholesterol transport, then examine the two failed CETP inhibitors, torcetrapib and dalcetrapib, to extract lessons for the field. With anacetrapib and evacetrapib in phase III development, the review attempts to differentiate these newer agents from their failed predecessors, framing whether pharmacologic CETP inhibition will ultimately reduce cardiovascular disease risk as one of the most important open questions in cardiovascular medicine.
Original abstract
The cholesteryl ester transfer protein (CETP) plays an integral role in the metabolism of plasma lipoproteins. Despite two failures, CETP inhibitors are still in clinical development. We review the genetics of CETP and coronary disease, preclinical data on CETP inhibition and atherosclerosis, and the effects of CETP inhibition on cholesterol efflux and reverse cholesterol transport. We discuss the two failed CETP inhibitors, torcetrapib and dalcetrapib, and attempt to extract lessons learned. Two CETP inhibitors, anacetrapib and evacetrapib, are in phase III development, and we attempt to differentiate them from the failed drugs. Whether pharmacologic CETP inhibition will reduce the risk of cardiovascular disease is one of the most fascinating and important questions in the field of cardiovascular medicine.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.