Plasma levels of high-density lipoprotein (HDL-C) cholesterol are inversely related to the incidence of coronary heart disease. The beneficial effects of HDL-C are thought to arise in part from its participation in reverse cholesterol transport (RCT), the process by which HDL-C shuttles cholesterol out of the atherosclerotic plaque to the liver for metabolism or elimination.The Merck CETP inhibitor anacetrapib has recently been shown to have robust effects on HDL-C and LDL-C in a Phase III clinical study (DEFINE trial). Sustained effects over 18 months were observed in patients with coronary heart disease and no adverse effects on blood pressure, electrolytes, and aldosterone levels were observed. The long term safety and efficacy of anacetrapib is being evaluated in a 30,000 patient global clinical outcomes study that is currently enrolling (REVEAL trial). The discovery, pre-clinical and clinical evaluation of anacetrapib will be described in detail.

Discovery and development of anacetrapib, a potent and orally active CETP inhibitor

243rd National Meeting (2012)

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