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Nacubactam is a novel small molecule beta-lactamase inhibitor developed to combat bacterial resistance to beta-lactam antibiotics. It acts through dual mechanisms of action: (1) inhibition of serine beta-lactamases (classes A and C and some class D), thereby protecting coadministered beta-lactams from enzymatic degradation; and (2) direct inhibition of penicillin binding protein 2 (PBP2) in Enterobacteriaceae, which impairs bacterial cell wall synthesis. Nacubactam is primarily being developed for use in combination with the carbapenem antibiotic meropenem for the treatment of serious gram-negative infections such as complicated urinary tract infections and pyelonephritis. The drug has demonstrated safety and tolerability in phase I studies and has advanced to phase III clinical trials[3][6][7].
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