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Cardiovasc Ther. 2011 Oct;29(5):327-39. doi: 10.1111/j.1755-5922.2010.00142.x. Epub 2010 Apr 9.

Anacetrapib: hope for CETP inhibitors?

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  • 1Robarts Research Institute and Schulich School of Medicine and Dentistry, University of Western Ontario, London, Ontario, Canada, N6A 5K8.


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.

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