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Anacetrapib is a small molecule cholesteryl ester transfer protein (CETP) inhibitor developed by Merck to treat hypercholesterolemia and prevent cardiovascular disease. It works by inhibiting CETP, a protein involved in the transfer of neutral lipids such as cholesteryl esters and triglycerides between lipoprotein particles. This inhibition raises high-density lipoprotein cholesterol (HDL-C) levels and lowers low-density lipoprotein cholesterol (LDL-C), thereby modifying lipid profiles to reduce cardiovascular risk. Anacetrapib was studied extensively in the large REVEAL clinical trial involving over 30,000 patients with atherosclerotic vascular disease already on statin therapy; it showed a significant reduction in major coronary events including coronary death, myocardial infarction, and coronary revascularization. Despite positive outcomes from REVEAL demonstrating cardiovascular benefit with good tolerability, Merck discontinued its development in 2017[1][3][5][6][9].
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