1842399-68-1

1842399-68-1 structure

Name: Ledaborbactam etzadroxil
Chemical Name: [(2-Ethylbutanoyl)oxy]methyl (3R)-2-hydroxy-3-(propionylamino)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylate
CAS Number: 1842399-68-1
Molecular Formula: C₁₉H₂₆BNO₇
Molecular Weight: 391.22
Catalog: Signaling Pathways Anti-infection Bacterial
Create Date: 2022-01-12 07:39:58
Modify Date: 2024-01-16 20:23:00
Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor[1].

Name	[(2-Ethylbutanoyl)oxy]methyl (3R)-2-hydroxy-3-(propionylamino)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylate
Synonyms	2H-1,2-Benzoxaborin-8-carboxylic acid, 3,4-dihydro-2-hydroxy-3-[(1-oxopropyl)amino]-, (2-ethyl-1-oxobutoxy)methyl ester, (3R)- [(2-Ethylbutanoyl)oxy]methyl (3R)-2-hydroxy-3-(propionylamino)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylate

Description	Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor[1].
Related Catalog	Research Areas >> Infection Signaling Pathways >> Anti-infection >> Bacterial
Target	β-Lactamase[1]
In Vivo	Upon dosing the Ledaborbactam etzadroxil (VNRX-7145) in mice, dogs, and monkeys, Ledaborbactam etzadroxil (5-10 mg/kg) demonstrates the most consistent oral bioavailability across species (F = 61-82%)[1]. In intestinal S9, Ledaborbactam etzadroxil is rapidly cleaved with short half-lives in all species with the exception of beagle dogs. The half-life in human plasma is short at about 11 min, which is closer to what was observed in the rodent species compared to the longer half-lives in dogs (43.9 min) and monkeys (22.0 min)[1]. In vivo efficacy is demonstrated in a lethal murine septicemia model by dosing Ledaborbactam etzadroxil (orally) with Ceftibuten. The ED50 value of 12.9 mg/kg[1].
References	[1]. Robert E Trout, et al. Discovery of VNRX-7145 (VNRX-5236 Etzadroxil): An Orally Bioavailable β-Lactamase Inhibitor for Enterobacterales Expressing Ambler Class A, C, and D Enzymes. J Med Chem. 2021 Jul 22;64(14):10155-10166.