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血管紧张素受体脑啡肽酶抑制剂 LCZ696:一种治疗动脉高血压的新型靶向治疗药物?

Angiotensin receptor neprilysin inhibitor LCZ696: a novel targeted therapy for arterial hypertension?

机构信息

Cardiology Department, Hippokration Hospital, Athens, Greece.

Department of Cardiology, Helena Venizelou Hospital, Athens, Greece.

出版信息

Eur Heart J Cardiovasc Pharmacother. 2015 Oct;1(4):260-4. doi: 10.1093/ehjcvp/pvv031. Epub 2015 Jul 8.

Abstract

The need for novel antihypertensive therapies represents a continuous challenge. LCZ696 is a first-in-class angiotensin receptor neprilysin inhibitor that has been shown to enhance endogenous natriuretic peptide (NP) actions on neurohormonal activation. This effect seems to be additive to that of the renin-angiotensin-aldosterone system (RAAS) suppression, as impressively suggested in the PARADIGM HF study. LCZ696 has been shown to be effective in reducing blood pressure in several small studies; however, its effectiveness and safety remain to be proved in larger studies. This review summarizes the role of RAAS and NP system in the pathophysiology of hypertension and reviews the current data on the antihypertensive effects of LCZ696.

摘要

新型抗高血压疗法的需求一直是一个挑战。LCZ696 是一种首创的血管紧张素受体脑啡肽酶抑制剂,已被证明可增强内源性利钠肽 (NP) 对神经激素激活的作用。这一效果似乎与肾素-血管紧张素-醛固酮系统 (RAAS) 的抑制作用相加,这在 PARADIGM HF 研究中得到了令人印象深刻的证明。几项小型研究表明 LCZ696 可有效降低血压;然而,其在更大规模研究中的有效性和安全性仍有待证实。本综述总结了 RAAS 和 NP 系统在高血压病理生理学中的作用,并回顾了 LCZ696 降压作用的现有数据。

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