Ibisobanuro

LCZ696 (Sacubitril / Valsartan), igizwe na Valsartan (ARB) na Sacubitril (AHU377) mu kigereranyo cya 1: 1, ni icyiciro cya mbere mu ishuri, bioavailable yo mu kanwa, hamwe na angiotensin reseptor-neprilysin (ARN) inhibitor ya hypertension no kunanirwa k'umutima [1] [2] [3]. LCZ696 itunganya umutima wa diabete yumutima mu guhagarika umuriro, guhagarika umutima hamwe na apoptose.

Amavu n'amavuko

LCZ696 niyambere mubyiciro bya ARNi (angiotensin reseptor neprilysin inhibitor) igizwe na anionic moieties ya AR valsartan 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 ari peptide ya bioactive ya sisitemu ya renin - angiotensin. Neprilysin ni endopeptidase idafite aho ibogamiye itesha agaciro peptide ya endogenous vasoactive peptide 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 bushingiye ku gukingira indwara ya peptide ya natriuretic natriuretic iterwa no kubuza neprilysin. Muri hypertensive double transgenic imbeba, LCZ696 yatumye igabanuka ryinshi kandi rigabanuka ryumuvuduko ukabije wa arterial. Abitabiriye ubuzima bwiza, ubushakashatsi butemewe, buhumye-buhumyi, ubushakashatsi bugenzurwa na platbo bwemeje ko LCZ696 yatanze icyarimwe hamwe na 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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