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Entresto
ENTRESTO inhibits neprilysin to increase natriuretic peptides while blocking AT1 angiotensin II receptors to reduce angiotensin II effects in heart failure.
At a glance
| Generic name | Entresto |
|---|---|
| Also known as | Entresto Tablets, Valsartan/sacubitril, valsartan/sacubitril, ARNI, Neprilysin inhibibitor |
| Sponsor | Novartis Pharmaceuticals |
| Modality | Small molecule |
| Therapeutic area | Other |
| Phase | FDA-approved |
Mechanism of action
ENTRESTO is a dual-action agent combining sacubitril (a neprilysin inhibitor prodrug) and valsartan (an AT1 receptor antagonist). Sacubitril is metabolized to LBQ657, which inhibits neprilysin (neutral endopeptidase), preventing degradation of natriuretic peptides and other cardioprotective peptides. Simultaneously, valsartan selectively blocks AT1 receptors, inhibiting angiotensin II-mediated vasoconstriction and aldosterone release. This complementary mechanism increases beneficial peptide levels while suppressing the renin-angiotensin-aldosterone system, resulting in improved cardiovascular and renal hemodynamics in heart failure patients.
Approved indications
Boxed warnings
- WARNING: FETAL TOXICITY When pregnancy is detected, discontinue ENTRESTO as soon as possible (5.1) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus (5.1) WARNING: FETAL TOXICITY See full prescribing information for complete boxed warning. When pregnancy is detected, discontinue ENTRESTO as soon as possible. ( 5.1 ) Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. ( 5.1 )
Common side effects
- Hypotension
- Hyperkalemia
- Cough
- Dizziness
- Renal failure
- Renal dysfunction
- Orthostasis
- Falls
- Serum creatinine increase >50%
- Hemoglobin/hematocrit decrease >20%
Serious adverse events
- Angioedema
- Angioedema in Black patients
Key clinical trials
- Efficacy and Safety of Sacubitril/Valsartan in African American Patients With Heart Failure With Reduced Ejection Fraction
- Manganese-enhanced Magnetic Resonance Imaging in Takotsubo Cardiomyopathy (NA)
- Bioequivalence Study of Sacubitril Alisartan Amlodipine Tablets (PHASE1)
- Mechanisms Underlying Hypotensive Response to ARB/NEP Inhibition - Aim 3 (PHASE4)
- Treating Heart Dysfunction Related to Cancer Therapy With Sacubitril/Valsartan (PHASE1, PHASE2)
- A Real-world Study of Clinical Treatment Guidelines for Patients With Heart Failure With Reduced Ejection Fraction Treated With Sacubitril/Valsartan
- A Safety and Tolerability Study of HJB647 in Heart Failure Participants With Reduced Ejection Fraction (PHASE1)
- A Real-world Study of the Effectiveness of Angiotensin Receptor-Neprilysin Inhibitor Therapy in Hypertensive Patients in the United Arab Emirates
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Entresto CI brief — competitive landscape report
- Entresto updates RSS · CI watch RSS
- Novartis Pharmaceuticals portfolio CI