The drug, called a CETP inhibitor, works by blocking the action of the cholesteryl ester transfer protein, which is known to lower HDL (the “good” cholesterol).
“CETP represents an important target because this protein plays a key role in HDL metabolism. In fact, a genetic deficiency of CETP is the main reason for high HDL in Asian populations,” says study author John Kastelein, M.D., Ph.D., from the Academic Medical Center in Amsterdam, The Netherlands.
The study was designed as a 12-week, multi-center, randomized trial evaluating the efficacy and safety of three different doses of the drug. A clear dose-dependent decrease in CETP activity was observed after one week, reaching a maximum decrease of 37 percent from baseline in the high-dose group after four weeks. After four weeks, participants taking the highest dose, 900 mg, had a 33.9 percent increase in HDL levels.
Except for some mild gastrointestinal side-effects, there were no major adverse effects from the new drug.
“Although these results hold promise, further studies are needed to investigate whether the increase in HDL cholesterol translates into a reduction in coronary artery disease risk,” says Kastelein.
Co-authors include Greetje J. de Grooth, M.D.; Jan Albert Kuivenhoven, Ph.D.; Anton F. H. Stalenhoef, M.D., Ph.D.; Jacqueline de Graaf, M.D., Ph.D.; Aeilko H. Zwinderman, Ph.D.; Jan L. Posma, M.D., Ph.D.; and Arie van Tol, Ph.D.
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