LDL and apoB
Thyromimetic T-0681 cuts atherosclerosis 80% in rabbits by raising hepatic LDL receptors, not by changing CETP (J Lipid Res 2008)
Original title: The thyromimetic T-0681 protects from atherosclerosis
In hyperlipidemic New Zealand White rabbits on high-cholesterol chow, prolonged treatment with the liver-selective thyromimetic T-0681 increased hepatic expression of both the LDL receptor and scavenger receptor class B type I, without affecting cholesteryl ester transfer protein activity. This upregulation of hepatic lipoprotein receptors accompanied a marked drop in apoB-containing lipoproteins, with plasma cholesterol falling 60% and plasma triglyceride falling more than 70%. T-0681 reduced atherosclerosis development by 80%, suggesting liver-selective thyromimetics could be useful therapeutic agents against atherosclerosis, with the benefit mechanistically attributed to hepatic receptor upregulation rather than any change in CETP activity.
Original abstract
This report describes studies in hyperlipidemic New Zealand White (NZW) rabbits investigating the impact of the liver-selective thyromimetic T-0681 on lipoprotein metabolism and the development of atherosclerosis. Prolonged treatment with T-0681 increased the hepatic expression of both LDL receptor and scavenger receptor class B, type I without affecting cholesteryl ester transfer protein activity. Upregulation of hepatic lipoprotein receptors was accompanied by a marked decrease of apolipoprotein B-containing lipoproteins, reflected by a 60% reduction of plasma cholesterol and a >70% reduction of plasma triglyceride levels. Most importantly, T-0681 reduced the development of atherosclerosis by 80% in NZW rabbits on high-cholesterol chow. Our data suggest that liver-selective thyromimetics, such as T-0681, may prove to be useful therapeutic agents against the development of atherosclerosis in humans.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.