SKU: N092  / 
    CAS Number: 1452458-86-4

    Nacubactam

    Mex$3,675.00

    Nacubactam is broad-spectrum non-β-lactam antibiotic that is a β-lactamase inhibitor. It was developed by Meiji Seika Pharma (Tokyo, Japan). It can inhibit class A and C β-lactamases in vitro, and has minor class D activity. It is classified as a diazabicyclooctanone. Compared to avibactam, it has an additional aminoethoxy group attached to the carbamoyl side chain that is responsible for its antimicrobial activity. Nacubactam is soluble in DMSO.

    Mechanism of Action

    Nacubactam is an antibacterial that acts as a penicillin binding protein (specifically PBP2).

    Molecular Formula C9H16N4O7S
    Spectrum

    Nacubactam is active against Gram-negative bacteria including Enterobacteriaceae.

    Microbiology Applications Studies have shown that Nacubactam has an enhanced effect when in combination with β-lactam agents, and especially those that bind to other penicillin binding proteins (PBPs) (ie non-PBP2) such as Meropenem. When used meropenem, it enhances the spectrum of activity and also improves the stability against β-lactamases. Meropenem-Nacubactam acts synergistically, notably against meropenem-resistant isolates.
    References

    Asempa TE et al (2019) Efficacy of human-simulated epithelial lining fluid exposure of Meropenem-Nacubactam combination against class A serine β-Lactamase-producing Enterobacteriaceae in the neutropenic murine lung infection model. Antimicrob. Agents Chemother. 63(4):e02382-18 PMID 30670411

    Livermore DM, Mushtaq S, Warner M, Woodford N (2015) Activity of OP0595/β-lactam combinations against Gram-negative bacteria with extended-spectrum, AmpC and carbapenem-hydrolysing β-lactamases. J. Antimicrob. Chemother. 70(11):3032-3041 PMID 26311835

    Monogue ML et al (2018) In vivo efficacy of Meropenem with a novel mon-β-lactam-β-lactamase inhibitor, Nacubactam, against Gram-negative organisms exhibiting various resistance mechanisms in a murine complicated urinary tract infection model. Antimicrob. Agents Chemother.62(9):e02596-17 PMID 30012751