Synonyms: VNRX-5236
Compound class:
Synthetic organic
Comment: Ledaborbactam (VNRX-5236) is a novel broad-spectrum boronic acid β-lactamase inhibitor (BLI). It is a reversible covalent inhibitor of serine β-lactamases (classes A, C, D) [1].
Ledaborbactam etzadroxil (VNRX-7145, PubChem CID 138455030), an orally bioavailable prodrug of ledaborbactam [3], is being developed in combination with ceftibuten for the treatment of infections caused by drug-resistant Enterobacterales. |
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Bioactivity Comments |
Ledaborbactam demonstrates inhibitory activity against serine β-lactamases from Ambler A, C, and D classes, including the carbapenemases KPC-2 (IC50 = 0.08 μM) and OXA-48 (IC50 = 0.32 μM) [1]. It restores the antibacterial activity of ceftibuten against strains of Enterobacterales expressing clinically important extended spectrum β-lactamases (ESBLs) and serine carbapenemases [1-2]. |