In 2015, the FDA first approved Novartis’ Entresto (sacubitril and valsartan). It contains a combination of sacubitril, a first-in-class neprilysin inhibitor, and valsartan, an angiotensin II antagonist.
Entresto is classified as an Angiotensin Receptor Neprilysin Inhibitor (ARNI) and is used in adults to reduce the risk of death and hospitalization in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction.
After you take Entresto, it is broken down into sacubitril and valsartan and absorbed into your body. Sacubitril is a “prodrug”, meaning it is inactive when taken, but it is further broken down to an active compound known as LBQ657.
After twice-daily dosing of Entresto, steady state levels of sacubitril, LBQ657, and valsartan are reached in 3 days, according to the manufacturer. Steady state is the time during which the concentration of the drug in the body stays consistent. In other words, steady state is when the rate of the drug going into your body is equal to the rate of drug elimination. You can take Entresto with or without food as this won’t affect its absorption or overall effect.
Although steady state levels are reached in 3 days, clinical effectiveness with Entresto will vary from person to person and may take longer due to unique factors such as age, weight, body fluid, other medications taken, kidney or liver function, or other medical conditions. Your doctor knows your medical condition the best and can give you specific information on your overall response to Entresto.
In clinical studies in patients with chronic heart failure, Entresto reduced hospitalizations and death when compared to other drugs commonly used for this condition, such as ACE inhibitors given alone. Clinically, Entresto is used with other standard heart failure medications such as beta-blockers, mineralocorticoid antagonists and other types of diuretics.