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首个血管紧张素受体-脑啡肽酶双重抑制剂—Entresto(sacubitril/缬沙坦) 被引量:7

A First-in-class angiotensin II receptor-neprilysin inhibitor(ARNi)Entresto(sacubitril/valsartan)
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摘要 Entresto(sacubitril/缬沙坦)是诺华公司研制的由脑啡肽酶(neprilysin)抑制剂sacubitril和血管紧张素II受体阻断剂缬沙坦组成的一种复方制剂,2015年7月FDA批准其用于治疗射血分数降低(Hfr EF)的心力衰竭,以降低心血管死亡和心衰住院风险。Entresto是首个也是唯一在临床试验中疗效显著超越标准治疗药物依那普利(enalapril)的药物,其可在增强心脏保护性神经内分泌系统(钠尿肽)的同时抑制有害的肾素-血管紧张素-醛固酮系统(RAAS)。Entresto被认为是近10年来心脏病治疗领域最重要的进展之一。笔者就Entresto的基本性质、作用机制、药动学、药效学、临床试验及应用等研发动态作一概述,以期能为医院临床用药起到指导作用。 Entresto(sacubitril/valsartan) is the first angiotensin II receptor-neprilysin inhibitor developed by Novartis,which has been approved by FDA for the treatment of heart failure with reduced ejection fraction(HFr EF) to reduce risk of cardiovascular death and hospitalization caused by heart failure. It acts to enhance the protective cardiac neurohormonal systems(NP system) while simultaneously suppressing the harmful RAAS system. Entresto is the first and only treatment to show a significant mortality benefit in a head-to-head trial against ACE-inhibitor enalapril with better safety.And it is considered to be one of the most important progress in the area of cardiology because of its outstanding performance. The properties, mechanism, pharmacokinetics, pharmacodynamics, clinical trials and applications of Entresto were reviewed in this article so as to guide clinical medication.
作者 王宏亮 王欢
出处 《临床药物治疗杂志》 2015年第6期85-88,共4页 Clinical Medication Journal
关键词 Etresto 血管紧张素受体-脑啡肽酶抑制剂 心力衰竭 Entrsto angiotensin II receptor-neprilysin inhibitor heart failure
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参考文献6

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共引文献89

同被引文献43

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