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心力衰竭的缬沙坦-沙库巴曲固定剂量复方制剂聚焦：迄今的证据

Spotlight on valsartan-sacubitril fixed-dose combination for heart failure: the evidence to date.

作者信息

Vilela-Martin José Fernando

机构信息

Internal Medicine Department, São José do Rio Preto State Medical School (FAMERP), São José do Rio Preto, Brazil.

出版信息

Drug Des Devel Ther. 2016 May 9;10:1627-39. doi: 10.2147/DDDT.S84782. eCollection 2016.

DOI:10.2147/DDDT.S84782
PMID:27274196
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4869613/
Abstract

Heart failure is a global problem with elevated prevalence, and it is associated with substantial cardiovascular morbidity and mortality. Treating heart-failure patients has been a very challenging task. This review highlights the main pharmacological developments in the field of heart failure with reduced ejection fraction, giving emphasis to a drug that has a dual-acting inhibition of the neprilysin and renin-angiotensin-aldosterone system. Neprilysin is an enzyme that participates in the breakdown of biologically active natriuretic peptides and several other vasoactive compounds. The inhibition of neprilysin has been a therapeutic target for several drugs tested in cardiovascular disease, mainly for heart failure and/or hypertension. However, side effects and a lack of efficacy led to discontinuation of their development. LCZ696 is a first-in-class neprilysin- and angiotensin-receptor inhibitor that has been developed for use in heart failure. This drug is composed of two molecular moieties in a single crystalline complex: a neprilysin-inhibitor prodrug (sacubitril) and the angiotensin-receptor blocker (valsartan). The PARADIGM-HF trial demonstrated that this drug was superior to an angiotensin-converting enzyme inhibitor (enalapril) in reducing mortality in patients with heart failure with reduced ejection fraction. The ability to block the angiotensin receptor and augment the endogenous natriuretic peptide system provides a distinctive mechanism of action in cardiovascular disease.

摘要

心力衰竭是一个全球患病率不断上升的问题，它与大量心血管疾病的发病率和死亡率相关。治疗心力衰竭患者一直是一项极具挑战性的任务。本综述重点介绍了射血分数降低的心力衰竭领域的主要药理学进展，着重介绍了一种对中性肽链内切酶和肾素 - 血管紧张素 - 醛固酮系统具有双重抑制作用的药物。中性肽链内切酶是一种参与生物活性利钠肽和其他几种血管活性化合物分解的酶。抑制中性肽链内切酶一直是在心血管疾病中测试的几种药物的治疗靶点，主要用于心力衰竭和 / 或高血压。然而，副作用和缺乏疗效导致它们的研发终止。LCZ696是一种一流的中性肽链内切酶和血管紧张素受体抑制剂，已被开发用于治疗心力衰竭。这种药物由单一晶体复合物中的两个分子部分组成：一种中性肽链内切酶抑制剂前体药物（沙库巴曲）和血管紧张素受体阻滞剂（缬沙坦）。PARADIGM - HF试验表明，在降低射血分数降低的心力衰竭患者的死亡率方面，这种药物优于血管紧张素转换酶抑制剂（依那普利）。阻断血管紧张素受体和增强内源性利钠肽系统的能力为心血管疾病提供了独特的作用机制。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e1b/4869613/9db0180ac6ce/dddt-10-1627Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e1b/4869613/f0ce0fe94026/dddt-10-1627Fig1.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e1b/4869613/9db0180ac6ce/dddt-10-1627Fig5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e1b/4869613/f0ce0fe94026/dddt-10-1627Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e1b/4869613/79f766fbf388/dddt-10-1627Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e1b/4869613/60d439cad0f1/dddt-10-1627Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e1b/4869613/fe09e76f69ea/dddt-10-1627Fig4.jpg
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In Reply: The PARADIGM-HF trial.回复：PARADIGM-HF试验。
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To the Editor: The PARADIGM-HF trial.致编辑：PARADIGM-HF试验。
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Influence of Ejection Fraction on Outcomes and Efficacy of Sacubitril/Valsartan (LCZ696) in Heart Failure with Reduced Ejection Fraction: The Prospective Comparison of ARNI with ACEI to Determine Impact on Global Mortality and Morbidity in Heart Failure (PARADIGM-HF) Trial.
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