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Obicetrapib is an orally bioavailable, highly selective small molecule inhibitor of cholesteryl ester transfer protein (CETP). It is being developed primarily for the treatment of dyslipidemia and hypercholesterolemia, particularly as an adjunct to maximally tolerated lipid-lowering therapies in patients with atherosclerotic cardiovascular disease (ASCVD) or heterozygous familial hypercholesterolemia (HeFH). By inhibiting CETP, obicetrapib reduces the transfer of cholesteryl esters from high-density lipoprotein (HDL) to apolipoprotein B-containing lipoproteins such as low-density lipoprotein cholesterol (LDL-C), resulting in significant reductions in LDL-C and other atherogenic lipid biomarkers. Clinical trials have shown that obicetrapib can lower LDL-C by up to 51% when added to statins and also increase HDL-C levels. Obicetrapib has demonstrated favorable safety and tolerability profiles in clinical studies. It is also under investigation for potential benefits in Alzheimer’s disease due to its effects on cholesterol metabolism in the brain[1][2][4][5].
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