The class
Review weighs CETP inhibition's physiology and animal-to-human evidence as a candidate route to raising HDL cholesterol (Curr Atheroscler Rep 2004)
Original title: Inhibition of cholesteryl ester transfer protein activity: a new therapeutic approach to raising high-density lipoprotein
This review examines whether CETP inhibition might one day join the clinical armamentarium for treating dyslipidemia and atherosclerotic vascular disease. Motivated by the inverse association between HDL cholesterol and atherosclerotic cardiovascular disease risk, the article reviews CETP's physiology within lipoprotein metabolism and surveys the animal and human data bearing on whether inhibiting CETP can both raise HDL cholesterol and reduce levels of atherogenic lipoproteins, framing CETP inhibition as a novel strategy still awaiting definitive clinical validation.
Original abstract
High-density lipoprotein (HDL) cholesterol levels are inversely associated with risk of atherosclerotic cardiovascular disease (ASCVD), leading to the concept that pharmacologic therapy to raise HDL cholesterol levels may reduce ASCVD risk. There is substantial interest in the concept of inhibition of the cholesteryl ester transfer protein (CETP) as a novel strategy for raising HDL cholesterol levels, as well as reducing levels of atherogenic lipoproteins. This article reviews the physiology of CETP in lipoprotein metabolism and the data in animals and humans that are relevant to the question of whether CETP inhibition may some day be part of the clinical armamentarium for treating dyslipidemia and atherosclerotic vascular disease.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.