Fa'amatalaga

LCZ696 (Sacubitril/Valsartan), e aofia ai Valsartan (o le ARB) ma le Sacubitril (AHU377) i le 1:1 molar ratio, o se muamua-i-vasega, tuufofoga bioavailable, ma lua-gaioioiga angiotensin receptor-neprilysin (ARN) inhibitor mo le toto maualuga. ma le faaletonu o le fatu[1][2][3].LCZ696 faʻaleleia le maʻisuka cardiomyopathy e ala i le taofia o le mumū, faʻamaʻi faʻamaʻi ma apoptosis.

Talaaga

O le LCZ696 e muamua i le vasega ARNi (angiotensin receptor neprilysin inhibitor) e aofia ai vaega anionic o AR valsartan ma le neprilysin inhibitor prodrug AHU377 (1:1 ratio) mo le faaletonu o le fatu ma le toto maualuga.

O le angiotensin receptors o G-protein-coupled receptors.Latou te faʻafesoʻotaʻi le cardiovascular ma isi aʻafiaga o le angiotensin II o se peptide bioactive o le renin-angiotensin system.Neprilysin ose endopeptidase le fa'aituau lea e fa'aleagaina peptides vasoactive endogenous pei o peptides natriuretic.O le taofiofia o le neprilysin e faʻateleina ai le faʻaogaina o peptide natriuretic lea na fesoasoani i le puipuiga o le fatu, fatugaʻo ma fatu.[1]

I isumu Sprague-Dawley, o le tautala tautala o le LCZ696 na taʻitaʻia ai le maualuga o le faʻaogaina o le faʻaogaina o le immunoreactivity o le atrial natriuretic peptide e mafua mai i le neprilysin inhibition.I isumu transgenic lua toto maualuga, LCZ696 na mafua ai le faʻalagolago i fualaʻau ma faʻaitiitia faʻaitiitiga o le mamafa o le toto.O tagata soifua maloloina o loʻo auai, o se suʻesuʻega faʻafuaseʻi, lua-tauaso, placebo-pulea suʻesuʻega na faʻamaonia ai o le LCZ696 na tuʻuina atu faʻatasi le neprilysin inhibition ma AT1 receptor blockade.LCZ696 sa saogalemu ma fa'apalepale lelei i tagata.[2] [3]

Fa'asinomaga:
McMurray JJ, Packer M, Desai AS et al.Angiotensin-neprilysin inhibition versus enalapril i le fatu faaletonu.N Egelani J Med.2014 Sep 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al.Pharmacokinetics ma pharmacodynamics o le LCZ696, o se tala fou e lua-gaioiga angiotensin receptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Ape;50(4):401-14.
Langenickel TH, Dole WP.Angiotensin receptor-neprilysin inhibition ma le LCZ696: o se auala fou mo le togafitia o le faaletonu o le fatu, Drug Discov Today: Ther Strategies (2014),

Teuina

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