cetpinhibition.org

Torcetrapib

A review argues the torcetrapib failure highlighted the gap between HDL cholesterol levels and HDL anti-inflammatory function (J Clin Lipidol 2007)

Original title: Peptide Mimetics of Apolipoproteins Improve HDL Function

J Clin Lipidol · · 4

Navab M, Anantharamaiah GM, Reddy ST, Van Lenten BJ, Buga GM, Fogelman AM

This review examines evidence that the anti-inflammatory properties of HDL may be at least as important as HDL cholesterol levels themselves, noting that the recent failure of torcetrapib clinical trials highlighted the potential differences between HDL cholesterol levels and actual HDL function. The authors argue that agents improving HDL function, including its anti-inflammatory properties, offer a therapeutic strategy for atherosclerosis and other chronic inflammatory conditions related to dyslipidemia distinct from simply raising HDL cholesterol. Drawing on the structure of plasma apolipoproteins, researchers have created peptide mimetics that improve HDL anti-inflammatory properties, reduce lesions, and improve vascular inflammation and function in animal atherosclerosis models without necessarily altering HDL cholesterol levels, with some now entering clinical pharmacologic studies.

Read the paper (DOI)PubMed

Original abstract

Over the past decade evidence has accumulated that suggests that the anti-inflammatory properties of HDL may be at least as important as the levels of HDL-cholesterol. The recent failure of the torcetrapib clinical trails has highlighted the potential differences between HDL-cholesterol levels and HDL function. Agents to improve HDL function including HDL anti-inflammatory properties provide a new therapeutic strategy for ameliorating atherosclerosis and other chronic inflammatory conditions related to dyslipidemia. Seeking guidance from the structure of the apolipoproteins of the plasma lipoproteins has allowed the creation of a series of polypeptides that have interesting functionality with therapeutic implications. In animal models of atherosclerosis, peptide mimetics of apolipoproteins have been shown to improve the anti-inflammatory properties of HDL, significantly reduce lesions and improve vascular inflammation and function without necessarily altering HDL-cholesterol levels. Some of these are now entering the clinical arena as interventions in pharmacologic and pharmacodynamic studies.

HDL biologytorcetrapib

Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.