Sacubitril

Category: pharmacological

Aliases: Component of Entresto

Pharmacological Mechanism

Neprilysin inhibitor prodrug — active metabolite LBQ657 inhibits NEP, raising natriuretic peptides (BNP, ANP) → vasodilation, natriuresis, anti-fibrotic. Always co-formulated with valsartan as Entresto for HFrEF; ACE inhibitor washout 36h required to avoid angioedema.

Half-Life (t½)

PO: 11h

Dosing Guidelines

• PO: Typical 49 mg (Range: 24–97 mg)

Target Organ Systems

• cardiovascular

Pathways It Modulates

• Bradykinin / kallikrein-kinin system (inhibitor) — NEP/neprilysin → ↑bradykinin + ↑natriuretic peptides
• Vasodilator pharmacology (inhibitor) — neprilysin (NEP)

Chemical Identifiers

• PubChem CID: 9811834
• Formula: C24H29NO5
• Molecular weight: 411.49 g/mol
• InChIKey: PYNXFZCZUAOOQC-UTKZUKDTSA-N
• SMILES: CCOC(=O)[C@H](C)C[C@@H](CC1=CC=C(C=C1)C2=CC=CC=C2)NC(=O)CCC(=O)O

References

• PMID 28527109