Sobetirome: A Selective Thyromimetic for the Treatment of Dyslipidemia
Ivan Tancevski, Egon Demetz and Philipp Eller
Affiliation: Department of Internal Medicine Medical University of Innsbruck, Anichstr. 35, 6020 Innsbruck, Austria.
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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