Dalcetrapib is a potent CETP modulator. It is a thioester pro-drug that is rapidly hydrolyzed to generate a pharmacologically active thiol. Dalcetrapib modulates cholesteryl ester transfer protein (CETP) activity to raise high-density lipoprotein cholesterol (HDL-C). It achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM.