Avibactam sodium

Avibactam sodium is a β-lactamase inhibitor that does not include the β-lactam core but maintains the capacity to covalently acylate its β-lactamase targets. Avibactam sodium inhibits β-lactamases CTX-M-15 and TEM-1, with IC50 values of 5 and 8 nM, respectively. β-Lactamases are enzymes produced by bacteria, with the ability to inactivate β-lactam antibiotics by hydrolyzing the β-lactam ring. β-Lactamases are responsible for resistance to penicillins, monobactams, carbapenems, and extended-spectrum cephalosporins. Avibactam sodium combined with β-lactam antibiotics can be potentially used for the treatment of bacterial infections comprising Gram-negative organisms.

References:

1. Ehmann DE, Jahić H, Ross PL, et al. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. Proceedings of the National Academy of Sciences of the United States of America, 2012, 109(29): 11663-11668.

2. Drawz SM, Bonomo RA. Three decades of beta-lactamase inhibitors. Clinical Microbiology Reviews, 2010, 23(1): 160-201.

3. Berkhout J, Melchers MJ, van Mil AC, et al. Pharmacokinetics and penetration of ceftazidime and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrobial Agents and Chemotherapy, 2015, 59(4): 2299-2304.