Brand Name: Entresto
Generic Name: sacubitril and valsartan
Medication Class: angiotensin receptor-neprilysin inhibitor (ARNi)
Manufacturer: Novartis Pharmaceuticals
FDA Approval Date: July 7, 2015
What is Entresto and its mechanism of action?
Entresto is an oral combination heart failure medication that contains sacubitril and valsartan. It belongs to a new class of medications called angiotensin receptor-neprilysin inhibitors (ARNi). Neprilysin (neutral endopeptidase) is an enzyme that destroys natriuretic peptides and bradykinin. Bradykinin and natriuretic peptides dilate blood vessels, reduce sodium and water retention, and provide other beneficial effects in heart failure patients.
Sacubitril is a prodrug that is converted into LBQ657 in the body. A prodrug is a molecule that is first converted to the active form of the drug via enzymes or a chemical transformation before it is effective. LBQ657 blocks the effect of neprilysin. Blocking the action of neprilysin increases the levels of natriuretic peptides and bradykinin, resulting in vasodilation (dilation of arteries), decreased aldosterone levels, natriuresis (excretion of sodium), and diuresis (increased urination).
Valsartan is an angiotensin receptor blocker (ARB). It selectively blocks the AT1 receptor, which blocks the effect angiotensin II and aldosterone release. Valsartan causes dilation of blood vessels and excretion of sodium in urine.
The net effect of Entresto in people with heart failure is reduced blood pressure and volume as well as preventing fibrosis (the thickening of arteries and valves).
What is Entresto used for treating?
Entresto is used to treat patients with NYHA Class II-IV chronic heart failure with a low ejection fraction (less than 40%). Entresto reduces the risk of cardiovascular death and hospitalization due to heart failure.
Heart failure is a chronic condition that affects 5.1 million people in the US. Heart failure occurs when changes in the structure and function of the heart prevent it from pumping enough blood to the body. Heart attacks and hardening of heart valves can alter the structure and function of the heart and cause heart failure. Fifty percent of people with heart failure die within 5 years of diagnosis. Entresto helps reduce blood pressure, reduce blood volume, and prevents stiffening of the heart valves, all of which work together to decrease the symptoms of heart failure.
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