Active Ingredient History
Sacubitril is a prodrug neprilysin inhibitor used in combination with valsartan (sold under the brand name Entresto among others) to reduce the risk of cardiovascular events in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. It was approved under the FDA's priority review process for use in heart failure on July 7, 2015. Sacubitril's active metabolite, LBQ657 inhibits neprilysin, a neutral endopeptidase that would typically cleave natiuretic peptides such as atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and c-type natriuretic peptide (CNP). ANP and BNP are released under atrial and ventricle stress, which activate downstream receptors leading to vasodilation, natriuresis and diuresis. Under normal conditions, neprilysin breaks down other vasodilating peptides and also vasoconstrictors such as angiotensin I and II, endothelin-1 and peptide amyloid beta-protein. Inhibition of neprilysin therefore leads to reduced breakdown and increased concentration of endogenous natriuretic peptides in addition to increased levels of vasoconstricting hormones such as angiotensin II. NCATS
Combination drugs
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Angiotensin II Type 1 Receptor Blockers (Phase 4)
Angiotensin Receptor Antagonists (Phase 4)
Antihypertensive Agents (Phase 4)
Aortic Valve Insufficiency (Phase 2)
Arrhythmias, Cardiac (Phase 2)
Atrial Fibrillation (Phase 4)
Atrial Remodeling (Phase 2)
Blood Pressure (Phase 4)
Breast Diseases (Phase 4)
Breast Neoplasms (Phase 4)
Cardiomyopathy, Hypertrophic (Phase 2/Phase 3)
Cardiotoxicity (Phase 4)
Cardiovascular Diseases (Phase 4)
Chagas Cardiomyopathy (Phase 3)
Chagas Disease (Phase 4)
Chronic Kidney Disease-Mineral and Bone Disorder (Early Phase 1)
Connective Tissue Diseases (Phase 4)
COVID-19 (Phase 1/Phase 2)
Diabetes Mellitus (Phase 4)
Diabetes Mellitus, Type 2 (Phase 4)
Drugs, Investigational (Phase 4)
Endomyocardial Fibrosis (Phase 2)
Energy Metabolism (Phase 2)
Erectile Dysfunction (Phase 3)
Essential Hypertension (Phase 3)
Glucose Intolerance (Phase 4)
Hamartoma (Phase 4)
Healthy Volunteers (Phase 2)
Heart Defects, Congenital (Phase 2/Phase 3)
Heart Diseases (Phase 3)
Heart Failure, Diastolic (Phase 4)
Heart Failure, Systolic (Phase 4)
Hemodialysis, Home (Phase 4)
HIV Infections (Phase 2)
Hypertension (Phase 4)
Hypertension, Pulmonary (Phase 3)
Hypertension, Renal (Phase 3)
Hypertrophy, Left Ventricular (Phase 4)
Hypotension (Phase 4)
Insulin Resistance (Phase 2)
Kidney Diseases (Phase 2)
Kidney Failure, Chronic (Phase 4)
Liver Diseases (Phase 2)
Metabolic Diseases (Phase 2)
Metabolism (Phase 2)
Mitral Valve (Phase 4)
Mitral Valve Insufficiency (Phase 4)
Myocardial Infarction (Phase 4)
Myocardium (Phase 4)
Myositis (Phase 2)
Natriuretic Peptides (Phase 2/Phase 3)
Neoplasms (Phase 4)
Neoplasms, Second Primary (Phase 4)
Obesity (Phase 4)
Peripheral Arterial Disease (Phase 2)
Pharmacokinetics (Phase 2)
Prediabetic State (Phase 4)
Renal Dialysis (Phase 2)
Renal Insufficiency, Chronic (Phase 1/Phase 2)
Renin-Angiotensin System (Phase 2/Phase 3)
Shock, Cardiogenic (Phase 4)
ST Elevation Myocardial Infarction (Phase 3)
Thyroid Neoplasms (Early Phase 1)
Ventricular Dysfunction, Left (Phase 4)
Ventricular Remodeling (Phase 2)
| Trial | Phase | Start Date | Organizations | Indications |
|---|
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