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低密度脂蛋白胆固醇降低疗法:重点关注前蛋白转化酶枯草溶菌素/克新9型(PCSK9)抑制剂。

LDL cholesterol-lowering therapies: emphasis on proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors.

作者信息

Sabatel-Pérez F, García-Ropero A, Santos-Gallego C G, Urooj Zafar M, Badimón J J

机构信息

Atherothrombosis Research Unit, Mount Sinai Heart, Icahn School of Medicine at Mount Sinai, New York, New York, USA; Cardiology Deparment, Complejo Hospitalario de Toledo, Toledo, Spain.

Atherothrombosis Research Unit, Mount Sinai Heart, Icahn School of Medicine at Mount Sinai, New York, New York, USA.

出版信息

Drugs Today (Barc). 2019 May;55(5):329-344. doi: 10.1358/dot.2019.55.5.2976501.

Abstract

Atherosclerotic cardiovascular disease is the leading cause of death all over the world. Its etiopathogenesis involves many correlated processes, with hypercholesterolemia being one of the main risk factors. Several large clinical trials have established the association between low-density lipoprotein cholesterol (LDL-C) levels and cardiovascular events. With the aim to take control over high LDL-C levels, several drugs with different targets in the cholesterol pathway have been developed. Statins are the cornerstone of pharmacological lipid-lowering treatment, although they are not always successful in attaining the recommended LDL-C levels. Therefore, newer and more potent therapies have been developed, being prominent among them ezetimibe and especially the proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors. Recent trials with these new therapies have reaffirmed the theory of 'the lower, the better' when it comes to LDL-C levels, and 'the earlier, the better' when it comes to atherosclerotic physiopathology.

摘要

动脉粥样硬化性心血管疾病是全球主要的死亡原因。其发病机制涉及许多相关过程,高胆固醇血症是主要危险因素之一。几项大型临床试验证实了低密度脂蛋白胆固醇(LDL-C)水平与心血管事件之间的关联。为了控制高LDL-C水平,已开发出几种作用于胆固醇代谢途径中不同靶点的药物。他汀类药物是药物降脂治疗的基石,尽管它们在达到推荐的LDL-C水平方面并不总是成功的。因此,已开发出更新、更有效的疗法,其中突出的是依折麦布,尤其是前蛋白转化酶枯草溶菌素/kexin 9型(PCSK9)抑制剂。最近针对这些新疗法的试验再次证实了LDL-C水平 “越低越好”,以及动脉粥样硬化病理生理学 “越早治疗越好” 的理论。

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