JTT-705 -: Treatment of lipoprotein disorders cholesteryl ester transfer protein inhibitor

The need for novel treatments to treat atherosclerosis and its complications has led to the development of inhibitors of cholesteryl ester transfer protein (CETP). The pro- or antiatherogenic role of CETP has been an important matter of debate over the last 20 years. Despite this, efforts have been made to design new, potent and selective CETP inhibitors such as JTT-705. This compound significantly increases plasma high-density lipoprotein cholesterol (HDL-C) in normolipidemic and hyperlipiclemic rabbits. Importantly, administration of JTT-705 causes a marked reduction in the aortic arch atherosclerotic area in moderately, but not in severely hyperlipidemic rabbits. Moreover, in a phase II trial in humans with mild-hyperlipidemia, JTT-705 was shown to be safe and effective in decreasing CETP activity and raising HDL-C levels.