Anacetrapib
Review asks whether anacetrapib offers the greatest HDL-raising, LDL-lowering promise among CETP inhibitors (Cardiovasc Ther 2011)
Original title: Anacetrapib: hope for CETP inhibitors?
This review examines cholesteryl ester transfer protein (CETP) inhibition as an antiatherogenic strategy, focusing on anacetrapib among the CETP inhibitors then in development, including dalcetrapib and torcetrapib. The authors report that anacetrapib demonstrated the greatest HDL cholesterol-raising and LDL cholesterol-lowering potential of the class, and that phase I and phase II trials found anacetrapib well tolerated without the pressor effects associated with torcetrapib. The review briefly surveys HDL-C raising through CETP inhibition as a cardioprotective strategy, with a specific focus on the clinical development of anacetrapib.
Original abstract
Inhibition of cholesteryl ester transfer protein (CETP), a key protein involved in reverse cholesterol transport, can lead to increases in high-density lipoprotein cholesterol (HDL-C) levels and thus, is under evaluation as an antiatherogenic strategy. Several CETP inhibitors have been under development including anacetrapib, dalcetrapib, and torcetrapib. To date, anacetrapib demonstrates the greatest HDL-C raising and low-density lipoprotein cholesterol (LDL-C) lowering potential. Phase I and phase II trials with anacetrapib have revealed that anacetrapib is well-tolerated and does not seem to possess the pressor effects associated with torcetrapib. This article will briefly review the HDL-C raising through CETP inhibition as an antiatherogenic strategy with a specific focus on anacetrapib.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.