Avibactam is a non-β-lactam β-lactamase inhibitor that is available in combination with ceftazidime (Avycaz). This combination was approved by the FDA on February 25, 2015 for the treatment of complicated intra-abdominal infections in combination with metronidazole, and the treatment of complicated urinary tract infections, including pyelonephritis caused by antibiotic resistant-pathogens, including those caused by multi-drug resistant gram-negative bacterial pathogens.
*The following content is generated by AI and is for reference only.
Avibactam is a novel, non-beta-lactam inhibitor of Class A, C, and D beta-lactamases, designed to overcome bacterial resistance mechanisms that render traditional antibiotics ineffective. Chemically known as (2S)-4-azabicyclo[3.1.0]hexane-2-carboxylic acid, 6-amino-3-[(1-methylpyrrolidin-2-yl)carbonyl]-, its molecular formula is C8H12N2O3. The compound carries the CAS number 757933-79-2. Structurally distinct from conventional beta-lactamase inhibitors like clavulanic acid or tazobactam, avibactam functions through a reversible carbamylation mechanism. It covalently binds to the active site serine residue of specific beta-lactamase enzymes, effectively blocking their ability to hydrolyze beta-lactam antibiotics such as ceftazidime and cefepime. This unique mode of action allows it to inhibit a broad spectrum of enzymes, including Extended-Spectrum Beta-Lactamases (ESBLs) and AmpC beta-lactamases, without inducing significant resistance development over time.
Clinically, avibactam is primarily utilized in combination with ceftazidime to treat complicated intra-abdominal infections, complicated urinary tract infections, and hospital-acquired pneumonia, including ventilator-associated pneumonia caused by susceptible Gram-negative bacteria. Its efficacy is particularly critical against multidrug-resistant pathogens like *Klebsiella pneumoniae* and *Pseudomonas aeruginosa*, which produce enzymes that typically degrade standard cephalosporins. By restoring the activity of these companion antibiotics, avibactam extends the therapeutic window for treating severe, life-threatening infections where few alternatives exist. The drug is administered intravenously and has demonstrated high bioavailability when paired with its partner agent. As antibiotic resistance continues to escalate globally, avibactam represents a pivotal advancement in antimicrobial stewardship, offering a robust solution for combating resistant strains that threaten public health. Ongoing research explores its potential applications against other enzyme classes and in combination with newer beta-lactam agents to further expand its clinical utility against emerging superbugs.