China LCZ696 (Sacubitril + Valsartan) artifices et praebitores

LCZ696(Sacubitril + Valsartan)

Brevis descriptio:

API Nomen	Indicium	Specification	US DMF	EU DMF	CEP
LCZ696(Sacubitril + Valsartan)	Cordis defectum	In-Domus	√

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Descriptio

LCZ696 (Sacubitril/Valsartan), Valsartan (ARB) et Sacubitrilum (AHU377) in 1, 1, molares ratio est prima in-genus, ore bioavailable, 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 peptide bioactiva systematis renin-angiotensini. Neprilysin neutrum est endopeptidasa quae peptides vasoactivas endogenas deponit sicut peptides natriureticae. Inhibitio neprilysin auget intentionem 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 proveniens. Duplex hypertensiva in muribus transgenicis, LCZ696 dosem dependens et reductionem in media pressione arteriarum sustentata effecit. Participes sano, temere obcaecati, placebo continenti studium confirmaverunt LCZ696, si concurrentes neprilysin inhibitionis et AT1 receptaculum obsidionis praebebant. LCZ696 tutus et bene toleratus in homine. [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);

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