The class
Review surveys CETP as a pivotal HDL-raising drug target as human CETP inhibitor data become available (J Lipid Res 2004)
Original title: A review of CETP and its relation to atherosclerosis
Noting that effective therapeutics for selectively raising HDL cholesterol remained unavailable despite HDL's well-documented atheroprotective role, this review positions CETP as a pivotal target for new HDL-raising drugs. It highlights that genetic CETP deficiency is the main cause of high HDL-c levels in Asian populations, underscoring CETP's central role in HDL metabolism, and notes that data on CETP inhibitors raising HDL-c in humans had just been published, with atherosclerosis outcome data expected soon. The review discusses the potential for CETP inhibitors to protect against atherosclerosis in light of current knowledge of CETP function in both rodents and humans.
Original abstract
Although the atheroprotective role of HDL cholesterol (HDL-c) is well documented, effective therapeutics to selectively increase plasma HDL-c levels are not yet available. Recent progress in unraveling human HDL metabolism has fuelled the development of strategies to decrease the incidence and progression of coronary artery disease (CAD) by raising HDL-c. In this quest for novel drugs, cholesteryl ester transfer protein (CETP) represents a pivotal target. The role of this plasma protein in HDL metabolism is highlighted by the discovery that genetic CETP deficiency is the main cause of high HDL-c levels in Asian populations. The use of CETP inhibitors to effectively increase HDL-c concentration in humans was recently published and data with regard to the effect on human atherosclerosis are expected shortly. This review discusses the potential of CETP inhibitors to protect against atherosclerosis in the context of the current knowledge of CETP function in both rodents and humans.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.