Descriptio

LCZ696 (Sacubitril/Valsartan), Valsartan (ARB) et Sacubitrilis (AHU377) in 1:1 molaris ratio est prima in-genus, ore liquabilis, et angiotensin receptor-neprilysin (ARN) inhibitor hypertensionis in genere. et cor defectum[1][2][3].LCZ696 meliorat cardiomyopathy diabeticam inhibendo inflammationem, accentus oxidativa et apoptosin.

Background

LCZ696 est prima in genere ARNi (angiotensin receptor neprilysin inhibitor) comprehendens medietatem anionicae valsartanae et neprilysin inhibitoris prodrug AHU377 (1:1 ratio) propter defectum cordis et hypertensionem.

Receptores angiotensin sunt G-dapibus receptores copulati.Mediant cardiovasculares aliosque effectus angiotensin II qui est peptidium bioactivum systematis renin-angiotensini.Neprilysin neutrum est endopeptidasa quae peptides vasoactivas endogenas deponit sicut peptides natriureticae.Inhibitio neprilysin auget unionem peptidum natriureticam quae ad tutelam cardiaci, vascularis et renalis contulit.[1]

In Sprague-Dawley mures, administratio oralis LCZ696 ad dosem dependens ortum duxit in immunoreactivity peptide atrialis natriureticae, ex inhibitione neprilysin orta.In duplice transgenico mures hypertensivo, LCZ696 dosem dependens et reductionem in media pressione arteriarum sustentata effecit.Sodales sanus, temere, duplex caecus, studium moderatum placebo confirmavit LCZ696, si concurrentem neprilysin inhibitionis et AT1 receptaculum obsidionis praebebat.LCZ696 tutus et bene toleratus in rebus humanis.[2] [3]

Notae:
McMurray JJ, Packer M, Desai AS et al.Angiotensin-neprilysin inhibitionis versus enalapril in cordis defectione.N Engl J Med.2014 Sep 11, 371 (11): 993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al.Pharmacokinetica et pharmacodynamica LCZ696, nove dual-agens angiotensin receptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Apr;
Langenickel TH, Dole WP.Angiotensin receptor-neprilysin inhibitionis cum LCZ696: accessus novus pro defectu curationis cordis, Drug Discov Hodie: Ther Strategies (2014);

Repono

Chemical structure