Ledaborbactam etzadroxil  (Synonyms: VNRX-7145)

Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor^[1].

β-Lactamase^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

391.22

C₁₉H₂₆BNO₇

1842399-68-1

CCC(CC)C(OCOC(C1=C2C(C[C@@H](B(O2)O)NC(CC)=O)=CC=C1)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]