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Sacubitril

沙庫巴曲
Mechanism of action:
Sacubitril 是一種腦啡肽酶抑制劑(neprilysin inhibitor)。Sacubitril 為前軀藥,在體內需代謝成具有活性的 sacubitrilat。腦啡肽酶(neprilysin)負責分解多種具保護作用的血管活性胜肽,包括心房利尿鈉肽(atrial natriuretic peptide)、腦利鈉利尿胜肽(brain natriuretic peptide)等。當腦啡肽酶受到 sacubitrilat 抑制後,血管活性胜肽分解減少,可產生血管擴張、利鈉與利尿作用、抑制心肌纖維化與心室重塑等。
Reference(s):
1. Gu J et al. (2010). Pharmacokinetics and pharmacodynamics of LCZ696, a novel dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol.
2. Mills J et al. (2015). The Role of Neprilysin Inhibitors in Cardiovascular Disease. Curr Heart Fail Rep.
3. King JB et al. (2015). Neprilysin Inhibition in Heart Failure with Reduced Ejection Fraction: A Clinical Review. Pharmacotherapy.
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