Focus on the Novel Cardiovascular Drug LZC696: from Evidence to Clinical Consideration

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• 作者：L. M. Lin ; Y. Wu ; M. F. Wu ; J. X. Lin
• 关键词：LCZ696 ; Sacubitril/valsartan ; Angiotensin receptor neprilysin inhibitor ; Heart failure ; Hypertension
• 刊名：Cardiovascular Drugs and Therapy
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：30
• 期：6
• 页码：623-633
• 全文大小：
• 刊物类别：Medicine
• 刊物主题：Cardiology;
• 出版者：Springer US
• ISSN：1573-7241
• 卷排序：30

文摘

LCZ696, a first-in-class angiotensin receptor neprilysin inhibitor (ARNI), is comprised of the angiotensin receptor blocker valsartan and the neprilysin inhibitor pro-drug sacubitril (AHU377). After oral administration, AHU377 is rapidly metabolized to the active neprilysin inhibitor LBQ657. LCZ696 exerts its effects of diuresis, natriuresis, vasodilation and aldosterone secretion inhibition through simultaneous renin-angiotensin-aldosterone system (RAAS) blockade and natriuretic peptides system (NPS) enhancement. Powerful evidence including PARAMETER and PRARDIGM-HF trials have shown that LCZ696 outperforms RAAS inhibition in treating patients with hypertension and heart failure with reduced ejection fraction (HFrEF), and is well tolerated. In addition, accumulating evidence also suggests its potential use in heart failure with preserved ejection fraction (HFpEF), chronic kidney disease (CKD), post-myocardium infarction (post-MI) and stroke. Both the FDA and CHMP have approved LCZ696 for treatment of HFrEF. Despite all this, some special issues (e.g. use in specific subgroups, adverse events, contraindications and cost-effectiveness analysis) should be considered before its implementation in clinical practice.