Penson Peter, McGowan Mary, Banach Maciej
a School of Pharmacy and Biomolecular Sciences , Liverpool John Moores University , Liverpool , UK.
b Esperion Therapeutics, Inc. , Ann Arbor , MI , USA.
Expert Opin Investig Drugs. 2017 Feb;26(2):251-259. doi: 10.1080/13543784.2017.1280458. Epub 2017 Jan 17.
Despite the effectiveness of statins in the treatment of lipid disorders, residual risk still exists, and hitherto studies where additional drugs were added to statin therapy have been mainly negative or the outcomes were very modest. Therefore there is still a need for new and effective oral agents in the combination therapy of lipid disorders. Areas covered: The review covers the current state of knowledge on the mechanism of action of bempedoic acid (ETC-1002) and results from recent clinical studies. Expert opinion: ETC-1002 is a novel oral lipid-lowering therapy. The reduction of both low-density lipoprotein cholesterol (LDL-C) and high sensitivity C-reactive protein (hsCRP) demonstrated by ETC-1002 in clinical trials suggests that agent may have the potential for CV risk reduction. Adverse effects of current lipid-lowering agents can be dose-limiting, and combination approaches to lipid-lowering may often be utilized for optimal CV risk reduction. Because of this, new lipid-modulating drugs are urgently required. ETC-1002 has a unique mechanism of action (adenosine triphosphate-citrate lyase inhibition). It has been shown to be safe in combination with statins as well as ezetimibe, and appears to effectively lower LDL-C and has the potential to reduce the risk of muscle-related adverse events, which can limit the utilization and effectiveness of statin therapy.
尽管他汀类药物在治疗脂质紊乱方面有效,但残余风险仍然存在,并且迄今为止,在他汀类药物治疗中添加其他药物的研究主要为阴性结果或效果甚微。因此,在脂质紊乱的联合治疗中仍然需要新的有效口服药物。涵盖领域:本综述涵盖了关于贝派地酸(ETC-1002)作用机制的当前知识状态以及近期临床研究的结果。专家意见:ETC-1002是一种新型口服降脂疗法。ETC-1002在临床试验中显示出对低密度脂蛋白胆固醇(LDL-C)和高敏C反应蛋白(hsCRP)的降低作用,表明该药物可能具有降低心血管风险的潜力。当前降脂药物的不良反应可能会限制剂量,并且降脂的联合方法可能经常用于最佳地降低心血管风险。因此,迫切需要新的脂质调节药物。ETC-1002具有独特的作用机制(抑制三磷酸腺苷 - 柠檬酸裂解酶)。已证明它与他汀类药物以及依折麦布联合使用是安全的,并且似乎能有效降低LDL-C,并有潜力降低与肌肉相关的不良事件风险,而这些不良事件会限制他汀类药物治疗的应用和效果。