Valsartan Sacubitril

CAS 936623-90-4

About the API

Systematic name Octadecasodiumhexakis(4-{[(1S,3R)-1-([1,1´-biphenyl]-4-ylmethyl)-4-ethoxy-3-methyl-4-oxobutyl]amino}-4-oxobutanoate)hexakis(N-pentanoyl-N-{[2´-(1H-tetrazol-1-id-5-yl)[1,1´-biphenyl]-4-yl]methyl}-L-valinate)—water (1/15).
Trade name(s) Entresto, LCZ696
Technology Synthetic Organic Chemistry
Molecular Formula C48H55N6O8Na3 2.5 H2O
Molecular Weight 957.99 g/mol
Physical properties White to almost white crystalline powder
Therapeutic category Cardiovascular
Available formulations Oral Solid
Regulations US DMF Flag US DMF

General Information

The combination of valsartan and sacubitril constitutes a novel strategy to reduce the risk of death and hospitalization due to heart failure. It is used in patients with chronic heart failure and reduced ejection fraction for almost all severity levels of heart failure (except for the lowest, level I, by New York Heart Association Functional Classification). Ejection fraction is a measurement for assessing the heart’s ability to pump out blood and for diagnosing and monitoring heart failure.

A twice-a-day tablet, the oral combination acts to enhance protective factors (natriuretic peptides) while simultaneously suppressing the damaging effects of the renin-angiotensin-aldosterone system (the RAAS).

The valsartan-sacubitril complex is usually administered in conjunction with other heart failure therapies, and can replace an angiotensin converting enzyme (ACE) inhibitor. It was shown to reduce the rate of cardiovascular death and hospitalizations related to heart failure compared to the substance enalapril. 

 

Developed by Novartis, the valsartan/sacubitril combination was approved by the FDA in 2015 under the trade name Entresto after being granted fast track designation. Each compound is prepared by multi-step chemical synthesis. The complex is a 1:1 mixture.