Anacetrapib: Hope for CETP Inhibitors?

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.