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Ledaborbactam is a novel, broad-spectrum boronic acid β-lactamase inhibitor that acts as a reversible covalent inhibitor of serine β-lactamases, specifically targeting Ambler class A, C, and D enzymes. It is being developed primarily as an orally bioavailable prodrug (ledaborbactam etzadroxil, formerly VNRX-7145), which is rapidly converted in vivo to the active compound. Ledaborbactam restores the activity of ceftibuten (an oral third-generation cephalosporin) against multidrug-resistant Enterobacterales producing serine β-lactamases—including ESBLs, KPCs, OXA-type carbapenemases, and class C enzymes. The main clinical focus has been on complicated urinary tract infections caused by drug-resistant Enterobacterales. Development and clinical trials are being conducted by Venatorx Pharmaceuticals[1][4][5][7].
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