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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 a Novartis company developed by the neprilysin inhibitor sacubitril and angiotensin II receptor antagonist valsartan a compound that the FDA approved in July 2015 It is used to treat heart failure with reduced ejection fraction (Hfr EF) to reduce the risk of cardiovascular death and hospitalizations for heart failure. Entresto is the first and only drug that significantly outperforms the standard treatment enalapril in clinical trials that enhances the protective neuroendocrine system (natriuretic peptide) of the heart while inhibiting unwanted renin-vascular Tensin - aldosterone system (RAAS). Entresto is considered as one of the most important advances in the field of heart disease in the past 10 years. The author gives an overview of the basic properties of Entresto, mechanism of action, pharmacokinetics, pharmacodynamics, clinical trials and application research developments in order to guide the clinical use of the drug in the hospital.