LCZ696(Sacubitril + Valsartan)
Tsanangudzo
LCZ696 (Sacubitril/Valsartan), inosanganisira Valsartan (an ARB) uye Sacubitril (AHU377) mu1: 1 molar ratio, ndeyekutanga-mu-kirasi, nemuromo bioavailable, uye mbiri-acting angiotensin receptor-neprilysin (ARN) inhibitor ye hypertension. uye kutadza kwemoyo[1][2][3].LCZ696 inosimbisa chirwere cheshuga chemoyo nekudzivirira kuzvimba, oxidative kusagadzikana uye apoptosis.
Background
LCZ696 ndiyo yekutanga mukirasi ARNi (angiotensin receptor neprilysin inhibitor) inosanganisira anionic moieties yeAR valsartan uye neprilysin inhibitor prodrug AHU377 (1: 1 ratio) yekushaya simba kwemoyo uye hypertension.
Iyo angiotensin receptors iG-protein-akabatana receptors.Vanopindirana nemoyo uye zvimwe zvinokonzerwa neangiotensin II inova bioactive peptide ye renin-angiotensin system.Neprilysin inonzi endopeptidase isina kwayakarerekera iyo inokanganisa endogenous vasoactive peptides yakadai se natriuretic peptides.Inhibition ye neprilysin inowedzera iyo natriuretic peptides concentration iyo yakabatsira kumoyo, vascular uye renal kudzivirira.[1]
Mumakonzo eSprague-Dawley, kutonga kwemuromo kweLCZ696 kwakatungamira mukukwira-kunoenderana nedosi mukusagadzikana kweatrial natriuretic peptide inokonzerwa neprilysin inhibition.Mune hypertension kaviri transgenic rats, LCZ696 yakakonzera kutsamira kwedosi uye kwakaramba kuderedzwa mukurevesa arterial pressure.Vatori vechikamu vane hutano, chidzidzo chisina kujairika, chakapetwa kaviri, che placebo-chinodzorwa chakasimbisa kuti LCZ696 yakapa panguva imwechete neprilysin inhibition uye AT1 receptor blockade.LCZ696 yaive yakachengeteka uye yakatenderwa mumunhu.[2] [3]
References:
McMurray JJ, Packer M, Desai AS et al.Angiotensin-neprilysin inhibition inopesana neenalapril mukukundikana kwemoyo.N Engl J Med.2014 Sep 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al.Pharmacokinetics uye pharmacodynamics yeLCZ696, inoveli mbiri-inobata angiotensin receptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Kubvumbi50(4):401-14.
Langenickel TH, Dole WP.Angiotensin receptor-neprilysin inhibition neLCZ696: nzira itsva yekurapa kwekushaya mwoyo, Drug Discov Nhasi: Ther Strategies (2014),
Storage
| Upfu | -20°C | 3 years |
| 4°C | 2 years | |
| In solvent | -80°C | 6 mwedzi |
| -20°C | 1 mwedzi |
Chimiro chemakemikari
Proposal18Quality Consistency Evaluation mapurojekiti akatenderwa4,uye6mapurojekiti ari pasi pekubvumidzwa.
Yepamberi yepasirese yemhando manejimendi system yakaisa hwaro hwakasimba hwekutengesa.
Kutariswa kwemhando yepamusoro kunofamba kuburikidza nehupenyu hwese kutenderera kwechigadzirwa kuti ive nechokwadi chemhando nekurapa.
Professional Regulatory Affairs timu inotsigira zvinodiwa zvemhando panguva yekushandisa uye kunyoreswa.
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