LCZ696 (Sacubitril + Valsartan)
Bayani
LCZ696 (Sacubitril/Valsartan), ya ƙunshi Valsartan (an ARB) da Sacubitril (AHU377) a cikin 1: 1 molar rabo, shi ne na farko-in-aji, na baka bioavailable, da dual-aiki angiotensin receptor-neprilysin (ARN) hanawa ga hauhawar jini. da gazawar zuciya[1][2][3]. LCZ696 yana inganta cututtukan zuciya na ciwon sukari ta hanyar hana kumburi, damuwa na oxidative da apoptosis.
Fage
LCZ696 shine na farko a cikin aji ARNi (angiotensin receptor neprilysin inhibitor) wanda ya ƙunshi nau'ikan anionic na AR valsartan da neprilysin inhibitor prodrug AHU377 (1: 1 rabo) don gazawar zuciya da hauhawar jini.
Masu karɓar angiotensin su ne masu karɓa na G-protein-haɗe-haɗe. Suna yin sulhu da cututtukan zuciya da sauran tasirin angiotensin II wanda shine peptide bioactive na tsarin renin-angiotensin. Neprilysin shine endopeptidase mai tsaka tsaki wanda ke lalata peptides na vasoactive na endogenous kamar peptides na natriuretic. Hanawa neprilysin yana ƙara yawan ƙwayar peptides na natriuretic wanda ya ba da gudummawa ga kariyar zuciya, jijiyoyin jini da na koda. [1]
A cikin berayen Sprague-Dawley, gudanar da baki na LCZ696 ya haifar da hauhawar dogaro da kashi a cikin rigakafi na peptide na atrial natriuretic sakamakon hanawa neprilysin. A cikin berayen transgenic biyu masu hauhawar jini, LCZ696 ya haifar da dogaro da kashi da ci gaba a cikin matsananciyar bugun jini. Mahalarta lafiya, bazuwar, makafi biyu, binciken sarrafa wuribo ya tabbatar da cewa LCZ696 ya ba da hanawar neprilysin na lokaci guda da kuma toshewar mai karɓar AT1. LCZ696 yana da aminci kuma an jure shi sosai a cikin ɗan adam. [2] [3]
Magana:
McMurray JJ, Packer M, Desai AS et al. Angiotensin-neprilysin hanawa da enalapril a cikin gazawar zuciya. N Engl J Med. 2014 Satumba 11; 371 (11): 993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al. Pharmacokinetics da pharmacodynamics na LCZ696, wani labari dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Afrilu; 50 (4): 401-14.
Langenickel TH, Dole WP. Angiotensin receptor-neprilysin hanawa tare da LCZ696: sabon tsarin kula da cututtukan zuciya, Drug Discov Today: Ther Strategies (2014)
Adana
| Foda | -20°C | shekaru 3 |
| 4°C | shekaru 2 | |
| A cikin ƙarfi | -80°C | Wata 6 |
| -20°C | Wata 1 |
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