Outcomes trials
Review compares torcetrapib, evacetrapib, dalcetrapib and anacetrapib trial outcomes and the future of CETP inhibition (J Cardiovasc Pharmacol Ther 2017)
Original title: Cholesteryl Ester Transfer Protein Inhibitors: Trials and Tribulations
This review surveys cholesteryl ester transfer protein (CETP) as a drug target, tracing the scientific rationale from genetic studies linking CETP activity to cholesterol levels through the clinical development of torcetrapib, evacetrapib, dalcetrapib, and anacetrapib. Although CETP inhibitors reliably altered their targeted cholesterol markers, the authors note that recent phase 3 outcome trials showed limited benefit on cardiovascular outcomes when added to standard care. The review discusses the mechanistic rationale for CETP inhibition, compares findings across the four inhibitor trial programs, and considers the future outlook for the drug class.
Original abstract
The cholesteryl ester transfer protein (CETP) is a plasma protein that plays an important role in the transfer of lipids between plasma lipoproteins. The CETP inhibitors have been widely studied as a pharmacologic therapy to target plasma cholesterol in order to reduce the risk of atherosclerotic cardiovascular disease . Using CETP inhibitors as cholesterol modifiers was based on the genetic research that found correlations between CETP activity and cholesterol levels. Although CETP inhibitors are successful at altering targeted cholesterol markers, recent phase 3 outcome trials have shown limited benefit on cardiovascular outcomes when combined with the current standard of care. We discuss the science of CETP inhibition, compare the CETP inhibitors developed (torcetrapib, evacetrapib, dalcetrapib, and anacetrapib), the findings from the CETP inhibitor trials, and the future outlook for CETP inhibitors in cholesterol modification.
the classoutcomes trialspharmacology
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.