LCZ696(Sacubitril + Valsartan)
wehewehe
ʻO LCZ696 (Sacubitril/Valsartan), i komo ʻo Valsartan (he ARB) a me Sacubitril (AHU377) i ka ratio molar 1:1, he mea mua i ka papa, bioavailable waha, a me ka hana ʻelua angiotensin receptor-neprilysin (ARN) inhibitor no ka hypertension. a me ka puʻuwai puʻuwai[1][2][3]. Hoʻomaikaʻi ʻo LCZ696 i ka cardiomyopathy maʻi maʻi ma o ka pale ʻana i ka mumū, ke kaumaha oxidative a me ka apoptosis.
Kāpae
ʻO LCZ696 ka mea mua ma ka papa ARNi (angiotensin receptor neprilysin inhibitor) e komo pū ana me nā moieties anionic o AR valsartan a me ka neprilysin inhibitor prodrug AHU377 (1:1 ratio) no ka hāʻule ʻana o ka naʻau a me ke kiʻekiʻe.
ʻO nā mea i loaʻa i ka angiotensin he mau mea hoʻokipa G-protein-coupled. Hoʻopili lākou i ka cardiovascular a me nā hopena ʻē aʻe o ka angiotensin II kahi peptide bioactive o ka ʻōnaehana renin-angiotensin. ʻO Neprilysin kahi endopeptidase kūʻokoʻa e hoʻohaʻahaʻa i nā peptides vasoactive endogenous e like me nā peptides natriuretic. ʻO ka pale ʻana i ka neprilysin e hoʻonui i ka natriuretic peptides kaila i kōkua i ka mālama ʻana i ka naʻau, vascular a me ka renal. [1]
I nā ʻiole Sprague-Dawley, hoʻokele waha o LCZ696 i alakaʻi i ka piʻi ʻana o ka nui o ka immunoreactivity o ka peptide natriuretic atrial i hopena mai ka inhibition neprilysin. I loko o nā ʻiole transgenic pālua hypertensive, LCZ696 ka mea i hoʻemi ʻia ka nui o ke kaomi arterial mean. ʻO ka poʻe i komo i ke olakino, kahi haʻawina i hoʻopaʻa ʻia, ʻelua makapō, placebo-controlled study i hāʻawi ʻo LCZ696 i ka concurrent neprilysin inhibition a me AT1 receptor blockade. Ua palekana a ʻae ʻia ka LCZ696 i ke kanaka. [2] [3]
Kuhikuhi:
McMurray JJ, Packer M, Desai AS et al. ʻO ka Angiotensin-neprilysin inhibition versus enalapril i ka pau ʻole o ka naʻau. N Engl J Med. 2014 Sep 11;371(11):993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S et al. ʻO Pharmacokinetics a me ka lāʻau lapaʻau o LCZ696, kahi moʻolelo dual-acting angiotensin receptor-neprilysin inhibitor (ARNi). J Clin Pharmacol. 2010 Apr;50(4):401-14.
Langenickel TH, Dole WP. ʻO ka Angiotensin receptor-neprilysin inhibition me LCZ696: kahi ala hou no ka mālama ʻana i ka puʻuwai puʻuwai, Drug Discov Today: Ther Strategies (2014),
Waihona
| Pauda | -20°C | 3 makahiki |
| 4°C | 2 makahiki | |
| I ka solvent | -80°C | 6 mahina |
| -20°C | 1 mahina |
ʻO ke kinona
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