Cholesteryl ester transfer protein (CETP) is an exchange protein which transfers cholesteryl esters from HDL to VLDL, IDL, and LDL in exchange for triglycerides. Dalcetrapib is an inhibitor of CETP that exhibits an IC50 value of 9 μM for plasma CETP in rabbits. Inhibition of CETP by dalcetrapib in rabbits given an atherogenic diet leads to elevation of HDL, decreased VLDL, and attenuation of the induced atherosclerosis. In human subjects, dalcetrapib also inhibits CETP activity and increases plasma HDL levels but it does not reduce the risk of recurrent cardiovascular events.
