Chemistry:Nacubactam
Nacubactam is an investigational β-lactamase inhibitor being developed for the treatment of infections caused by carbapenem-resistant Enterobacteriaceae (CRE). It belongs to the diazabicyclooctane (DBO) class of compounds and exhibits a dual mechanism of action. Nacubactam inhibits serine β-lactamases, including classes A and C and some class D enzymes, while also directly inhibiting penicillin-binding protein 2 (PBP2) in Enterobacteriaceae.[1][2] This unique profile allows nacubactam to both protect partner β-lactam antibiotics from degradation and exert direct antibacterial effects. As of 2024, nacubactam is undergoing clinical trials in combination with other β-lactam antibiotics such as meropenem, cefepime, and aztreonam for the treatment of complicated urinary tract infections and other serious bacterial infections caused by multidrug-resistant pathogens.[3][4]
References
- ↑ "Safety and Pharmacokinetic Characterization of Nacubactam, a Novel β-Lactamase Inhibitor, Alone and in Combination with Meropenem, in Healthy Volunteers". Antimicrobial Agents and Chemotherapy 64 (5). April 2020. doi:10.1128/AAC.02229-19. PMID 32041717.
- ↑ "Development of an optimized and practical pharmacokinetics/pharmacodynamics analysis method for aztreonam/nacubactam against carbapenemase-producing K. pneumoniae". The Journal of Antimicrobial Chemotherapy 78 (4): 991–999. April 2023. doi:10.1093/jac/dkad033. PMID 36775998.
- ↑ "Nacubactam". DrugBank. https://go.drugbank.com/drugs/DB15353.
- ↑ "In Vivo Pharmacodynamics of β-Lactams/Nacubactam against Carbapenem-Resistant and/or Carbapenemase-Producing Enterobacter cloacae and Klebsiella pneumoniae in Murine Pneumonia Model". Antibiotics (Basel, Switzerland) 10 (10): 1179. September 2021. doi:10.3390/antibiotics10101179. PMID 34680760.
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