Ledaborbactam etzadroxil_product_DataBase

Bioactivity	Ledaborbactam etzadroxil (VNRX-7145) is an orally active Ambler class A, C, and D β-lactamase enzymes inhibitor[1].
Target	β-Lactamase
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].
Name	Ledaborbactam etzadroxil
CAS	1842399-68-1
Formula	C19H26BNO7
Molar Mass	391.22
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB