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Entresto

Novartis AG

Drug Names(s): LCZ696, valsartan/AHU377, valsartan and sacubitril, Neparvis (Europe)

Description: LCZ696 is an angiotensin receptor blocker/neutral endopeptidase (ARB/NEP) inhibitor . It is a single molecule comprising molecular moieties of valsartan and NEP inhibitor prodrug AHU377.

The simultaneous inhibition of ACE and NEP (vasopeptidase inhibition) results in increased vasodilation, decreased vasoconstriction, and a decrease in blood pressure and vascular tone.

Angiotensin receptor blockers (ARB) drugs block the chemical receptors for angiotensin II on the small arteries (arterioles). Therefore, the angiotensin cannot cause these arteries to constrict, which lowers the blood pressure. Angiotensin II is the most powerful constrictor of blood vessels. By blocking the action of angiotensin II on the small arteries, the ARB drugs prevent them from narrowing (constricting). The effect is to widen the arteries, which lowers the blood pressure.

Inhibitors of neutral endopeptidase, an enzyme that degrades a variety of vasoactive peptides, potentiate the natriuretic (secretion of sodium in the urine), the diuretic (excretion of urine), and the blood-pressure lowering effects of natriuretic peptides.

Inhibition of both would theoretically lead to reduced blood pressure in a broader range of conditions than either alone.


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