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Pactimibe is a small molecule drug that acts as a dual inhibitor of acyl-coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2). It was developed by Daiichi Sankyo for the treatment of atherosclerosis and coronary heart disease. The drug works by inhibiting cholesterol absorption from the intestine, reducing cholesteryl ester formation in the liver and macrophages, enhancing cholesterol elimination from the body, and inhibiting secretion of very low density lipoprotein cholesterol from the liver. These mechanisms contribute to its hypocholesterolemic and anti-atherosclerotic effects. Clinical development reached up to phase III trials for atherosclerosis but was discontinued due to lack of efficacy on secondary endpoints compared to standard care[3][4][5][6].
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