Description: Avibactam sodium hydrate (NXL104; NXL-104 hydrate; Avycaz), the sodium salt and hydrated form of avibactam, is a novel, potent, and covalent reversible non-β-lactam β-lactamase inhibitor with antibiotic activity. It inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively. Avibactam was approved for use in combination with ceftazidime by the FDA on February 25, 2015, for treating complicated urinary tract and complicated intra-abdominal Infections caused by antibiotic resistant-pathogens, including those caused by multi-drug resistant gram-negative bacterial pathogens.
References:
[1]. Ehmann DE, et al. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8.
[2]. Livermore DM, et al. Characterization of β-lactamase and porin mutants of Enterobacteriaceae selected with ceftaroline + avibactam (NXL104). J Antimicrob Chemother. 2012 Jun;67(6):1354-8.
[3]. Berkhout J, et al. Pharmacokinetics and penetration of GR20263 and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304.
[4]. Inhibition of Klebsiella β-Lactamases (SHV-1 and KPC-2) by Avibactam: A Structural Study. PLoS One. 2015 Sep 4;10(9):e0136813.
Related CAS #: 1192491-61-4 (sodium) 1192500-31-4 (free acid)