LCZ696(Sacubitril + Valsartan)
Tlhaloso
LCZ696 (Sacubitril/Valsartan), e nang le Valsartan (an ARB) le Sacubitril (AHU377) ka karolelano ea 1: 1 molar, ke ea pele-pele, ka molomo bioavailable, le dual-acting angiotensin receptor-neprilysin (ARN) inhibitor bakeng sa hypertension. le ho hloleha ha pelo [1][2][3].LCZ696 e matlafatsa lefu la pelo ea lefu la tsoekere ka ho thibela ho ruruha, khatello ea oxidative le apoptosis.
Ka morao
LCZ696 ke ea pele sehlopheng sa ARNi (angiotensin receptor neprilysin inhibitor) e nang le likarolo tsa anionic tsa AR valsartan le neprilysin inhibitor prodrug AHU377 (1: 1 ratio) bakeng sa ho hloleha ha pelo le khatello ea mali.
Li-angiotensin receptors ke li-receptor tsa G-protein tse kopantsoeng.Li kopanya methapo ea pelo le litlamorao tse ling tsa angiotensin II, e leng bioactive peptide ea sistimi ea renin-angiotensin.Neprilysin ke endopeptidase e sa nke lehlakore e senyang li-peptide tsa vasoactive tse kang li-peptide tsa natriuretic.Ho thibela neprilysin ho eketsa mahloriso a li-peptide tsa natriuretic tse tlatselitseng ts'ireletsong ea pelo, methapo le renal.[1]
Ho likhoto tsa Sprague-Dawley, tsamaiso ea molomo ea LCZ696 e lebisitse ho phahama ho itšetlehileng ka tekanyo ea immunoreactivity ea atrial natriuretic peptide e bakoang ke thibelo ea neprilysin.Likhotong tsa hypertensive tse peli tsa transgenic, LCZ696 e bakile ho fokotseha ho itšetlehileng ka tekanyo le ho tsitsitseng ho bolelang khatello ea mali.Barupeluoa ba phetseng hantle, thuto e laoloang ka mokhoa o sa reroang, e sa boneng habeli, e laoloang ke placebo e netefalitse hore LCZ696 e fane ka thibelo ea neprilysin ka nako e le 'ngoe le ho thibela li-receptor tsa AT1.LCZ696 e ne e bolokehile ebile e mamelloa hantle ho batho.[2] [3]
Litšupiso:
McMurray JJ, Packer M, Desai AS et al.Angiotensin-neprilysin inhibition khahlano le enalapril ka ho hloleha ha pelo.N Engl J Med.2014 Sep 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al.Pharmacokinetics le pharmacodynamics ea LCZ696, buka e ncha e sebetsang ka bobeli ea angiotensin receptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Apr;50(4):401-14.
Langenickel TH, Dole WP.Angiotensin receptor-neprilysin inhibition le LCZ696: mokhoa o mocha oa phekolo ea lefu la pelo, Drug Discov Today: Ther Strategies (2014),
Polokelo
| Phofo | -20°C | 3 lilemo |
| 4°C | lilemo tse 2 | |
| Ka solvent | -80°C | Likhoeli tse 6 |
| -20°C | 1 khoeli |
Sebopeho sa lik'hemik'hale
Tlhahiso18Merero ea Tlhahlobo ea Boleng e amohetsoeng4, le6merero e tlas'a tumello.
Sistimi e tsoetseng pele ea boleng ba machaba e thehile motheo o tiileng oa thekiso.
Tlhokomelo ea boleng e tsamaisana le potoloho eohle ea bophelo ba sehlahisoa ho netefatsa boleng le phello ea kalafo.
Sehlopha sa Litaba tsa Taolo ea Setsebi se tšehetsa litlhoko tsa boleng nakong ea kopo le ngoliso.
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