Promising data on new CETP inhibitor

Studies reported at the European Society of Cardiology Annual Congress, Vienna 2007 indicate that MK-0859, a new cholesteryl ester transfer protein (CETP) inhibitor, produces effective dose-dependent lipid-lowering and is well tolerated.1

In one study, 36 healthy volunteers were randomised to treatment with MK-0859 at doses of 50, 100, 200, 400 or 800 mg once-daily for 14 days with a meal, and 12 received placebo. Treatment with MK-0859 increased HDL cholesterol by 84-118% and lowered LDL cholesterol by 36-57%. CETP activity was also decreased by 34- 61%.

In the second study, patients with LDL cholesterol levels > 100 mg/dL (2.59 mmol/L) and <190 mg/dL (4.91 mmol/L) were randomised to treatment with MK-0859 10, 40, 150 or 300 mg once daily with a meal for 28 days (n=39) or placebo (n=9). MK-0859 produced dose-dependent increases in HDL cholesterol (by 41% with 10 mg to 129% with 300 mg), and decreases in LDL cholesterol (by 5% with 10 mg and 38% with 300 mg).

In both studies, MK-0859 was well tolerated. These preliminary data support further investigation in clinical settings.

References

1. Krishna R, Anderson MS, Jin B et al. Effect of the potent cholesteryl ester transfer protein (CETP) inhibitor, MK-0859, on lipoproteins in healthy subjects and in subjects with dyslipidemia. Eur Heart J 2007; 28 (abstract suppl):18. Abstract 321.