DS-8190a

DS-8190a is a novel, orally administered small-molecule activator of lecithin:cholesterol acyltransferase (LCAT) developed by Daiichi Sankyo. Unlike earlier covalent activators such as Compound A, DS-8190a binds to LCAT in a non-covalent and reversible manner, stabilizing the enzyme in its active conformation. By enhancing LCAT activity, the drug promotes the esterification of free cholesterol into cholesteryl esters within high-density lipoprotein (HDL) particles, thereby facilitating reverse cholesterol transport (RCT). Preclinical studies in cynomolgus monkeys and human LCAT-transgenic mice have demonstrated that DS-8190a increases HDL cholesterol levels, enhances cholesterol efflux from peripheral tissues, and significantly reduces atherosclerotic plaque accumulation. It is being investigated as a potential therapeutic for atherosclerosis and familial LCAT deficiency.

Other names

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