The class
Early phase I and II data show CETP inhibitors raise HDL-C by up to 70 percent, though effects on triglycerides remain unclear (Curr Opin Investig Drugs 2003)
Original title: Therapeutic implications of cholesteryl ester transfer protein inhibitors in hyperlipidemia and low high-density lipoprotein-cholesterolemia
Reviewing the therapeutic case for CETP inhibitors in hyperlipidemia and low HDL cholesterol, this article notes that CETP-lowering therapies have preventative effects against aortic atherosclerosis in cholesterol-fed rabbits, and that phase I and II clinical trial data show this new compound class can raise HDL-C by up to 70%. The authors judge CETP inhibitors likely to benefit patients with moderate hypercholesterolemia and HDL-C below 40 mg/dL, while cautioning that their effects on triglyceride metabolism were, at the time, still unknown and warranted further study before broader clinical use.
Original abstract
Low levels of high-density lipoprotein cholesterol (HDL-C) in plasma are an independent coronary risk factor. Therapies that lower cholesteryl ester transfer protein (CETP) have preventative effects on aortic atherosclerosis in cholesterol-fed rabbits. CETP inhibitors are a new class of compounds that can increase HDL-C levels by up to 70%, according to data from phase I and II clinical trials. CETP inhibitors are therefore likely to be beneficial in patients with moderate hypercholesterolemia and HDL-C levels lower than 40 mg/dl. CETP inhibitors should, however, be viewed with caution as their effects on triglyceride metabolism are currently unknown.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.