Vaborbactam

Vaborbactam is an inhibitor of β-lactamases (K_is = 29-110 nM for class A and class C enzymes).¹ It is selective for bacterial β-lactamases over a panel of mammalian serine proteases (IC₅₀s = ≥1,000 μM). Vaborbactam potentiates the activity of biapenem against K. pneumonia expressing the β-lactamase KPC-2, reducing the MIC value for biapenem from 32 to 1 μg/ml when used at a concentration of 0.02 μg/ml. It also potentiates the activity of the carbapenem antibiotics biapenem, meropenem (Item No. 16068), ertapenem, and imipenem (Item No. 16039) against clinical isolates of E. coli, E. cloacae, K. oxytoca, and K. pneumoniae that produce serine β-lactamases (MICs = ≤0.06-4 and 4-64 μg/ml in the presence and absence of vaborbactam, respectively). In vivo, vaborbactam (50 mg/kg) reduces the number of colony forming units (CFUs) in the lung in a neutropenic mouse lung infection model when used in combination with biapenem or meropenem. Formulations containing vaborbactam in combination with meropenem have been used for the treatment of carbapenem-resistant Enterobacteriaceae infections.

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1. Hecker, S.J., Reddy, K.R., Totrov, M., et al. Discovery of a cyclic boronic acid β-lactamase inhibitor (RPX7009) with utility vs class A serine carbapenemases. J. Med. Chem. 58(9), 3682-3692 (2015).