Sobetirome: a selective thyromimetic for the treatment of dyslipidemia.

Ivan Tancevski, Egon Demetz, Philipp Eller
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引用次数: 26

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.

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索比替罗:一种治疗血脂异常的选择性拟甲状腺药。
动脉粥样硬化及其临床后遗症仍然是西方社会死亡的主要原因。在过去的25年中,出现了一类新的药物来治疗血脂异常,这是冠状动脉疾病的主要危险因素:肝脏和甲状腺激素受体同种异构体β-选择性类似物。本文将讨论最近申请的sobetirome (GC-1)专利,该专利为建立降低血浆胆固醇和甘油三酯的新方法奠定了基础。我们将重点讨论赋予sobetirome降脂特性的主要机制,包括诱导肝脏LDL受体,促进所谓的逆向胆固醇转运,最后诱导胆汁酸的产生和胆汁固醇的分泌。总之,拟甲状腺药如索比替rome可能是治疗合并高脂血症的有效方法,合并高脂血症与主要的心血管风险相关。
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