Torcetrapib
A review of CETP molecular mechanisms notes the negative phase III torcetrapib trials challenged the future of the drug class (Cell Mol Life Sci 2010)
Original title: Cholesteryl ester transfer protein and its inhibition
This review examines cholesteryl ester transfer protein (CETP), which transfers cholesteryl esters from atheroprotective HDL to proatherogenic LDL and VLDL, thereby lowering HDL and raising LDL and VLDL levels. Although CETP inhibition is considered a potential dyslipidemia treatment, the review notes that the role of CETP-mediated lipid transfer in atherosclerosis, and the value of CETP inhibition for atherosclerosis prevention, has long been controversial. While many animal studies support the hypothesis that inhibiting CETP activity is beneficial, negative phase III clinical-endpoint trials with the CETP inhibitor torcetrapib challenged the future prospects of CETP inhibitors as therapeutic agents. The review provides an update on the molecular mechanisms of CETP activity and its inhibition.
Original abstract
Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the transfer of cholesteryl esters from the atheroprotective high density lipoprotein (HDL) to the proatherogenic low density lipoprotein cholesterol (LDL) and very low density lipoprotein cholesterol (VLDL) leading to lower levels of HDL but raising the levels of proatherogenic LDL and VLDL. Inhibition of CETP is considered a potential approach to treat dyslipidemia. However, discussions regarding the role of CETP-mediated lipid transfer in the development of atherosclerosis and CETP inhibition as a potential strategy for prevention of atherosclerosis have been controversial. Although many animal studies support the hypothesis that inhibition of CETP activity may be beneficial, negative phase III studies on clinical endpoints with the CETP inhibitor torcetrapib challenged the future perspectives of CETP inhibitors as potential therapeutic agents. The review provides an update on current understanding of the molecular mechanisms involved in CETP activity and its inhibition.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.