Sacubitril
Sacubitril. Neprilysin inhibitor prodrug — active metabolite LBQ657 inhibits NEP, raising natriuretic peptides (BNP, ANP) → vasodilation… Oral half-life 12 h.
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.
ANALYTE: SACUBITRILAT, discriminated against the parent by this record own other citation: sacubitril peaks at 0.5 h and shows "no accumulation" on twice-daily dosing while sacubitrilat peaks at 1.5-2.0 h and accumulates about 1.6-fold. So the stored 11 h cannot be the parent. Corrected to the verbatim 12 h from a healthy-subject arm. CITATION DEFECT: the previous source abstract supports none of the stored numbers — no half-life, no bioavailability, no volume, no rate. F 0.6 and V 75 remain unsourced and are gap-listed; ka 2.8 dropped. mw 411.49 is the sacubitril ethyl ester. MASS: the stored weight was the prodrug while the declared analyte is sacubitrilat — 7.3 percent high, the smallest of the series, and inert today. THE RECORD OWN NOTE ALREADY DISCLOSED IT; disclosure is not a fix. MY DOSE PRIOR IS REFUTED AND THE DOSE BLOCK IS RIGHT: the stored figures are the SACUBITRIL COMPONENTS of the combination tablet, stated verbatim in that form, and the molar ratio checks out. The half-life is verbatim from the healthy arm and correctly analyte-referenced. THE BIOAVAILABILITY AND VOLUME ARE UNSOURCEABLE, NOT MERELY UNSOURCED: seven papers were chased and every one reports peak times, half-life ranges, geometric-mean ratios, fold-changes or urinary recovery, NEVER an absolute bioavailability, clearance or volume. The stored bioavailability matches the label qualitative floor and nothing indexed. A CLASS-2 NEAR-MISS IS RECORDED SO NOBODY LATER MISTAKES IT FOR THE SOURCE: one paper reports a urinary recovery percentage close to the stored figure but not equal to it.
Pharmacokinetics
- Oral — t½ 12 h · F 60% · Vd 75 L
Sources: PMID:28527109, PMID:27230850