Sharaxaada

LCZ696 (Sacubitril/Valsartan), oo ka kooban Valsartan (an ARB) iyo Sacubitril (AHU377) ee 1: 1 saamiga molar, waa fasalka koowaad, afka laga heli karo, iyo dual-acting angiotensin receptor-neprilysin (ARN) inhibitor ee hypertension. iyo wadne xanuun[1][2][3]. LCZ696 waxay hagaajisaa wadnaha wadnaha ee sonkorowga iyadoo la xakameynayo bararka, cadaadiska oksaydhka iyo apoptosis.

Asalkii hore

LCZ696 waa kan ugu horreeya ee fasalka ARNi (angiotensin reseptor neprilysin inhibitor) oo ka kooban unugyada anionic ee AR valsartan iyo neprilysin inhibitor prodrug AHU377 (1: 1 ratio) ee wadne xanuunka iyo dhiig-karka.

Receptors-yaasha angiotensin waa G-protein-ku-xidhay-qabayaal. Waxay dhexdhexaadiyaan wadnaha iyo xididada iyo saamaynta kale ee angiotensin II kaas oo ah peptide bioactive ee nidaamka renin-angiotensin. Neprilysin waa endopeptidase dhexdhexaad ah oo hoos u dhigaya peptides-ka vasoactive-ka ah sida peptides natriuretic. Joojinta neprilysinku waxay kordhisaa diiradda peptides natriuretic taas oo gacan ka geysatay ilaalinta wadnaha, xididada iyo kelyaha. [1]

Jiirka Sprague-Dawley, maamulka afka ee LCZ696 wuxuu horseeday kor u kaca qiyaasta ku-tiirsanaanta difaaca jirka ee peptide atrial natriuretic oo ka dhashay xannibaadda neprilysin. Jiirka labajibbaaran ee hypertensive transgenic, LCZ696 waxay keentay qiyaas ku-tiirsanaan iyo hoos u dhac joogto ah oo ah cadaadiska celceliska halbowlaha. Ka-qaybgalayaasha caafimaadka qaba, kala-sooc, laba-indho la'aan, daraasad la xakameeyey placebo ayaa xaqiijisay in LCZ696 ay bixisay xannibaadda neprilysin-ka iyo xannibaadda soo-dhoweynta AT1. LCZ696 waxay ahayd badbaado oo si wanaagsan loogu dul-qaatay aadanaha. [2] [3]

Tixraacyo:
McMurray JJ, Packer M, Desai AS iyo al. Joojinta Angiotensin-neprilysin iyo enalapril ee wadnaha oo aan shaqeynin. N Engl J Med. 2014 Seb 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S iyo al. Pharmacokinetics iyo farmacodynamics ee LCZ696, oo ah laba jibbaar angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Abriil; 50 (4): 401-14.
Langenickel TH, Dole WP. Angiotensin receptor-neprilysin inhibition oo leh LCZ696: hab cusub oo loogu talagalay daaweynta wadnaha oo aan shaqeynin, Drug Discov Today: Ther Strategies (2014)

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