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Early review surveys progress toward antisense and small-molecule CETP inhibitors as HDL-raising therapies (Curr Opin Drug Discov Devel 2001)
Original title: The discovery of new cholesteryl ester transfer protein inhibitors
This review discusses CETP as an important but controversial target for raising HDL cholesterol and treating atherosclerosis, describing significant progress toward inhibiting the protein through an antisense inhibitor, irreversible small-molecule inhibitors and reversible small-molecule inhibitors. Several orally bioavailable small-molecule CETP inhibitors had shown potential to improve the HDL to LDL cholesterol ratio in various animal models at reasonable doses, with one compound demonstrating efficacy in preventing atherosclerosis in a rabbit model. The authors note that several more years of clinical testing would likely be needed to establish whether these candidates could provide therapeutic benefit to patients with coronary artery disease.
Original abstract
Cholesteryl ester transfer protein (CETP) has been an important but controversial target for elevating HDLc (high density lipoprotein cholesterol) and treating atherosclerosis. Significant progress toward inhibiting CETP has occurred on several fronts, including the development of an antisense inhibitor, irreversible small molecule inhibitors and reversible small molecule inhibitors. Several orally bioavailable, small molecule CETP inhibitors have shown potential to improve the HDLc to LDLc (low density lipoprotein cholesterol) ratio in various animal models at reasonable doses, and one of these compounds has shown efficacy in preventing atherosclerosis in a rabbit model. However, several more years of clinical testing will likely be needed to demonstrate that these clinical candidates can provide a potential therapeutic benefit to patients with coronary artery disease.
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Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.