A CEPT inhibitor (IC50s = 17 and 15 nM for CETP-dependent transfer of cholesterol esters and triglycerides, respectively); decreases plasma levels of LDL and triglycerides, reduces atherosclerotic lesion sizes, and increases HDL levels in the E3L.CETP mouse model of atherosclerosis; increases HDL levels by 2-fold and lowers LDL and fasting plasma triglyceride levels in rhesus macaques at 150 mg/kg,