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
|