脑啡肽酶抑制剂:心血管治疗领域的新利器

Neprilysin inhibition-the new cardiovascular therapeutic weapon

脑啡肽酶抑制剂(又称中性内肽酶抑制剂)是一种新型的,具有潜在改善患者心血管疾病转归的药物。脑啡肽酶抑制剂可增加钠尿肽系统活性,增加尿钠排泄、利尿以及抑制肾素-血管紧张素系统(RAS)的作用。因此,该药对慢性心衰、高血压和慢性肾病的RAS激活状态具有治疗作用。早期的脑啡肽酶抑制剂与血管紧张素转化酶抑制剂结合物由于其无法接受的血管性水肿发生率而终止。然而,新型的血管紧张素受体脑啡肽酶抑制剂——LCZ696,经大量的研究显示对心血管疾病具有有益作用。

Neprilysin inhibition（NEPi）,also known as neutral endopeptidase inhibition,is a new therapeutic strategy with potential to improve outcomes for patients with cardiovascular disease.NEPi enhances the activity of natriuretic peptide systems leading to natriuresis,diuresis and inhibition of the renin-angiotensin system（RAS）,which could act as a potentially beneficial counter-regulatory system in states of RAS activation such as chronic heart failure（HF）,hyper-tension and chronic kidney disease.Early NEPi drugs combined with angiotensin converting enzyme inhibitors were associated with unacceptable rates of angioedema and,therefore,withdrawn.However,a new class of drug called angiotensin receptor neprilysin inhibitor（ARNi）has been developed.One such drug,LCZ696,has shown substantial benefits in trials in cardiovascular disease.