eflucimibe

Eflucimibe (F12511) is a small molecule and potent, selective inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT, also known as SOAT1), an intracellular enzyme that catalyzes the formation of cholesteryl esters from cholesterol and fatty acid[5][7][6]. Developed as a hypocholesterolemic and anti-atherosclerotic agent, eflucimibe has been investigated primarily to reduce cholesterol absorption, prevent foam cell formation in atherosclerosis, and lower plasma lipid levels[2][6]. It demonstrates high-affinity inhibition of ACAT1 (Ki ≈ 39 nM), significantly reducing esterification of cholesterol in vitro and in vivo, and has passed phase 1 clinical safety trials in the context of anti-atherosclerosis[1][4][3]. Recent preclinical studies have also evaluated F12511 in nanoparticle/liposome formulations for potential use in neurodegenerative indications such as Alzheimer's disease, where ACAT inhibition may ameliorate amyloid and tau pathology[3][4].

Other names

eflucimibeF12511F-12511F 12511(S)-2′,3′,5′-trimethyl-4′-hydroxy-α-dodecylthioacetanilide