Anacetrapib
Review of new oral dyslipidaemia drugs names anacetrapib the only CETP antagonist that reduces cardiovascular events (Eur J Prev Cardiol 2020)
Original title: Recent advances in synthetic pharmacotherapies for dyslipidaemias
This review surveys new oral agents developed to address LDL cholesterol, triglycerides, and HDL cholesterol beyond statins and injectable biologics. For hypercholesterolaemia it highlights pitavastatin, a potent low-dose statin without adverse glucose effects, and bempedoic acid, which acts upstream of HMG-CoA reductase without muscular side effects. For hypertriglyceridaemia it covers pemafibrate, a selective PPAR-alpha agonist that does not raise homocysteine or creatinine, high-dose eicosapentaenoic ethyl ester, and gemcabene, which lowers both cholesterol and triglycerides by regulating apoB-100. Among cholesteryl ester transfer protein antagonists that raise HDL-C, the review specifically notes that only anacetrapib has been shown to reduce cardiovascular events, while probucol is discussed separately for stimulating reverse cholesteryl ester transport and stabilizing plaques.
Original abstract
Despite the demonstrated benefits of statins and injectable biologics, there is a need for new and safe oral agents for addressing classical lipid targets, low-density lipoprotein cholesterol (LDL-C), triglycerides and high-density lipoprotein cholesterol (HDL-C). LDL-C is unquestionably causal in the development of atherogenesis and atherosclerotic cardiovascular disease, but new options are required to address triglyceride-rich lipoproteins and lipoprotein(a). For hypercholesterolaemia, pitavastatin provides a very low dose and potent statin that does not adversely affect glucose metabolism; bempedoic acid acts at a biochemical step preceding hydroxymethylglutaryl-CoA reductase and is not associated with muscular side effects. For hypertriglyceridaemia, pemafibrate displays a unique and selective agonist activity on peroxisomal proliferator activated receptor-α that does not elevate homocysteine or creatinine. Although omega-3 fatty acids supplementation is not effective in secondary prevention, high dose eicosapentaenoic ethyl ester can lead to a remarkable fall in first and recurrent events in high risk patients with hypertriglyceridaemia/low HDL-C. Gemcabene, a dicarboxylic acid regulating apolipoprotein B-100, is effective in reducing both cholesterol and triglycerides. Among cholesteryl ester transfer protein antagonists that elevate HDL-C, only anacetrapib reduces cardiovascular events. Probucol stimulates reverse cholesteryl ester transport, lowers LDL-C stabilizing plaques and may lower incidence of cardiovascular events. These agents, which act through novel mechanisms, afford good and potentially safe treatment choices that may increase adherence and the attainment of therapeutic targets.
anacetrapibthe classpharmacology
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.