LCZ696(Sacubitril + Valsartan)

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LCZ696(Sacubitril + Valsartan) Te ngoikore o te ngakau Roto-whare    


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Whakaahuatanga

Ko te LCZ696 (Sacubitril/Valsartan), ko Valsartan (he ARB) me te Sacubitril (AHU377) i roto i te 1:1 ōwehenga molar, he tuatahi-i roto i te karaehe, he waatea-a-waha, me te angiotensin receptor-neprilysin (ARN) mahi-rua te aukati mo te whakaheke toto. me te ngoikore o te ngakau [1][2][3].Ko te LCZ696 te whakapai ake i te cardiomyopathy mate huka ma te aukati i te mumura, te ahotea oxidative me te apoptosis.

 

Papamuri

Ko te LCZ696 te tuatahi o te karaehe ARNi (angiotensin receptor neprilysin inhibitor) kei roto nga waahanga anionic o AR valsartan me te neprilysin inhibitor prodrug AHU377 (1:1 ōwehenga) mo te ngoikore o te ngakau me te whakaheke toto.

Ko nga kaiawhina angiotensin ko nga kaiwhakawhiwhi G-protein-coupled.Ka takawaenga ratou i te mate ngakau me etahi atu paanga o te angiotensin II he peptide koiora o te punaha renin-angiotensin.Ko te Neprilysin he endopeptidase kūpapa e whakaheke ana i nga peptides vasoactive endogenous penei i nga peptides natriuretic.Ko te aukati i te neprilysin ka whakanui ake i te kukū o nga peptides natriuretic i whai waahi ki te tiaki ngakau, ngakau me nga whatukuhu.[1]

I roto i nga kiore Sprague-Dawley, ko te whakahaere a-waha o LCZ696 i arahi ki te pikinga o te horopeta-whakaaro i te immunoreactivity o te peptide natriuretic atrial i hua mai i te aukati neprilysin.I roto i nga kiore whakaheke toto-rua, na te LCZ696 i pa mai te whakahekenga o te pehanga toto.Ko nga kaiuru hauora, he rangahau matapōkere, rua-matapo, placebo-whakahaere rangahau i whakapumautia e LCZ696 i whakarato i te aukati neprilysin i te wa kotahi me te aukati kaiwhakawhiwhi AT1.Ko te LCZ696 he haumaru, he pai te manawanui ki te tangata.[2] [3]

Tohutoro:
McMurray JJ, Packer M, Desai AS et al.Angiotensin-neprilysin inhibition versus enalapril i te ngoikore o te ngakau.N Ingarihi J Med.2014 Sep 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al.Pharmacokinetics me pharmacodynamics o LCZ696, he pukapuka-rua-mahi angiotensin receptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Apr;50(4):401-14.
Langenickel TH, Dole WP.Angiotensin receptor-neprilysin inhibition with LCZ696: a novel approach for the treatment of heart failure, Drug Discov Today: Ther Strategies (2014),

 

Rokiroki

Paura

-20°C

3 tau
 

4°C

2 tau
I te whakarewa

-80°C

6 marama
 

-20°C

1 marama

Hanganga matū

LCZ696(Sacubitril + Valsartan)

Tiwhikete

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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