Ibisobanuro

MC no kunanirwa k'umutima [1] [2] [3].LCZ696 itunganya indwara ya diabete yumutima hamwe no guhagarika umuriro, guhagarika umutima hamwe na apoptose.

Amavu n'amavuko

LCZ696 niyambere mubyiciro ARNi (angiotensin reseptor neprilysin inhibitor) igizwe na anionic moieties ya AR valsartan hamwe na neprilysin inhibitor prodrug AHU377 (1: 1 ratio) kubera kunanirwa k'umutima na hypertension.

Imiti ya angiotensin ni G-proteine-yakira.Bahuza umutima nimiyoboro nizindi ngaruka za angiotensin II arirwo peptide ya bioactive ya sisitemu ya renin - angiotensin.Neprilysin ni endopeptidase itabogamye itesha agaciro peptide ya endogenous vasoactive nka peptide natriuretic.Kubuza neprilysine byongera peptide ya natriuretic yagize uruhare mu kurinda umutima, imitsi ndetse no kurinda impyiko.[1]

Imbeba za Sprague-Dawley, ubuyobozi bwo mu kanwa bwa LCZ696 bwatumye ubwiyongere bukabije buterwa no gukingira indwara ya peptide natriuretic peptide iterwa no kubuza neprilysin.Muri hypertensive double transgenic imbeba, LCZ696 yateje igipimo gishingiye kandi ikomeza kugabanuka kumuvuduko ukabije wa arterial.Abitabiriye ubuzima bwiza, ubushakashatsi bwateganijwe, buhumye-buhumyi, ubushakashatsi bugenzurwa na platbo byemeje ko LCZ696 yatanze icyerekezo kimwe cya neprilysin hamwe no gukumira reseptor ya AT1.LCZ696 yari ifite umutekano kandi yihanganirwa neza mubantu.[2] [3]

Reba:
McMurray JJ, Packer M, Desai AS n'abandi.Angiotensin-neprilysin kubuza na enalapril kunanirwa k'umutima.N Engl J Med.2014 Nzeri 11; 371 (11): 993-1004.
Gu J, Noe A, Chandra P, Al-Fayoumi S n'abandi.Pharmacokinetics na pharmacodynamics ya LCZ696, igitabo gishya gikora angiotensin reseptor-neprilysin inhibitor (ARNi).J Clin Pharmacol.2010 Mata; 50 (4): 401-14.
Langenickel TH, Dole WP.Angiotensin reseptor-neprilysin kubuza hamwe na LCZ696: uburyo bushya bwo kuvura kunanirwa k'umutima, Ibiyobyabwenge Discov Uyu munsi: Ther Strategies (2014),

Ububiko

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