Ledaborbactam etzadroxil

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

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

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].

[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.