Abstract
Atherosclerosis and its clinical sequelae still represent the primary cause of death in Western societies. During the past 25 years, a novel drug class to treat dyslipidemia, a main risk factor for coronary artery disease, emerged: liver- and thyroid hormone receptor isoform β- selective analogs. The present review will discuss the recent patents applied for sobetirome (GC-1), which set the course for the establishment of a novel approach to lower plasma cholesterol and triglycerides. We will focus on the major mechanisms conferring sobetirome lipid-lowering properties, including the induction of hepatic LDL receptor, the promotion of the so-called reverse cholesterol transport, and finally the induction of bile acid production and biliary sterol secretion. In summary, thyromimetics such as sobetirome may represent a useful treatment for combined hyperlipidemia, which is associated with a major cardiovascular risk.
Keywords: GC-1, LDL cholesterol, reverse cholesterol transport, bile acids, triglycerides, atherosclerosis, coronary heart disease, dextrothyroxine, triiodothyronine, 3,5-dibromo-3'-pyrida-zinone-l-thyronine, L-94901, eprotirome, sobetirome, triiodo-thyronine, hypothyroidism, bradycardia, low density lipoprotein, hypercholesterolemic mice, apolipoprotein B, MB-07811, KB-141, T3, T-0681, CYP7A1, ABCG5, ABCG8, SREBP1
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