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ledaborbactam etzadroxil
- Development stage
- Phase 1
- Lead developer
- Venatorx Pharmaceuticals
- Modality
- Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Ledaborbactam etzadroxil is an orally bioavailable prodrug of the bicyclic boronate β-lactamase inhibitor ledaborbactam (formerly VNRX-5236). It is designed to inhibit Ambler class A, C, and D β-lactamases, thereby restoring the activity of oral cephalosporin antibiotics such as ceftibuten against multidrug-resistant (MDR) Enterobacterales. The drug acts by covalently and reversibly binding to the active site serine of these β-lactamases, preventing them from hydrolyzing β-lactam antibiotics. Ledaborbactam etzadroxil is being developed primarily in combination with ceftibuten for oral treatment of complicated urinary tract infections (cUTI), including those caused by carbapenem-resistant Enterobacteriaceae and extended-spectrum beta-lactamase-producing bacteria. The developer is VenatoRx Pharmaceuticals[1][4][5][6][8].
- Other names
- ledaborbactam etzadroxilUNII-C5F376EKS2UNII-C-5F376EKS2UNII-C 5F376EKS2
02
Targets
Neuraminidase
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