LCZ696, consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.

≥98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

奥帕曲拉；缬沙坦；Sacubitril；valsartan

white powder

DMSO : 28 mg/mL (30.6 mM)
Ethanol : 9 mg/mL (9.82 mM), warmed
Water : 92 mg/mL (100.4 mM)

RAAS

LCZ696 is a single molecule that is comprised of molecular moieties of valsartan, an ARB, and AHU377, a neprilysin inhibitor (1:1 ratio).

LCZ696 exerts a blood pressure lowering effect. Blood pressure reduction by LCZ696 is associated with a significant increase in urinary sodium excretion and sympathetic activity suppression. LCZ696 significantly ameliorates cardiac hypertrophy and inflammation, coronary arterial remodeling, and vascular endothelial dysfunction in high-salt loaded SHRcp compared with valsartan. The neprilysin inhibitor component of LCZ696, LBQ657, inhibits hypertrophy but not fibrosis. The angiotensin receptor blocker component of LCZ696, valsartan inhibits both hypertrophy and fibrosis. Dual valsartan+LBQ augment the inhibitory effects of valsartan and the highest doses completely abrogate angiotensin II-mediated effects. Pre-treatment with LCZ696 reduces the ischemic area. The decrease in cerebral blood flow in the peripheral region of the ischemic area is significantly attenuated by pre-treatment with LCZ696. LCZ696 pre-treatment significantly decreases the increase of superoxide anion production in the cortex on the ischemic side.