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

Upon administering Ledaborbactam etzadroxil (VNRX-7145) to mice, dogs, and monkeys, the compound consistently shows oral bioavailability (F = 61-82%) across these species, with dosages ranging from 5-10 mg/kg[1]. It is rapidly metabolized in the intestinal S9 fractions of all tested species, except for beagle dogs, displaying short half-lives. The human plasma half-life is notably brief at approximately 11 minutes, aligning more closely with rodents than with the longer half-lives observed in dogs (43.9 minutes) and monkeys (22.0 minutes)[1]. In vivo efficacy against lethal murine septicemia was achieved when Ledaborbactam etzadroxil was orally co-administered with Ceftibuten, yielding an ED50 value of 12.9 mg/kg[1].