Anacetrapib
Review asks whether anacetrapib is the last surviving CETP inhibitor as REVEAL results loom (Expert Opin Pharmacother 2016)
Original title: Anacetrapib for the treatment of dyslipidaemia: the last bastion of the cholesteryl ester transfer protein inhibitors?
This review examines anacetrapib after high-profile withdrawals of other cholesteryl ester transfer protein (CETP) inhibitors cast doubt on the class. Despite those setbacks, the authors report anacetrapib appears safe and well tolerated, delivering substantial increases in HDL cholesterol and reductions in LDL cholesterol as monotherapy and combined with a statin. The review covers CETP and HDL cholesterol as therapeutic targets, the pharmacokinetics and pharmacodynamics of anacetrapib, and recent trial data, noting the field's focus has shifted from HDL-raising to LDL-lowering because LDL and HDL functionality under CETP inhibition remain unclear. The authors conclude the phase III REVEAL trial will be decisive for whether anacetrapib earns a place in clinical care.
Original abstract
Introduction: Inhibition of cholesteryl ester transfer protein (CETP) has emerged as a potential way to decrease cardiovascular risk by raising high density lipoprotein (HDL) cholesterol and lowering low density lipoprotein (LDL) cholesterol concentrations. However, high profile withdrawals of several CETP inhibitors have cast doubt over this hypothesis. Despite this concern, anacetrapib appears to be safe, well-tolerated and delivers a substantial increases in HDL cholesterol and reductions in LDL cholesterol as monotherapy and when combined with a statin.
Areas Covered: We discuss the role of CETP and HDL cholesterol as therapeutic targets, describe the pharmacokinetics and pharmacodynamics of anacetrapib, as well as report on the recent clinical trials.
Expert Opinion: The focus of CETP inhibition has shifted from HDL cholesterol-raising to LDL cholesterol-lowering. Although anacetrapib appears to be safe and is effective in altering lipid-related biochemical parameters of interest, its effect on cardiovascular outcomes remains unknown. Extrapolation of LDL cholesterol lowering to improved cardiovascular outcomes is not possible, because LDL and HDL functionality in the setting of anacetrapib treatment is unclear. The results of the phase III REVEAL randomised controlled trial will be critical for anacetrapib to establish a place in clinical care.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.