piperacillin + enmetazobactam

Piperacillin + enmetazobactam is an investigational fixed-dose intravenous combination of the broad-spectrum ureidopenicillin antibiotic piperacillin with enmetazobactam, a novel diazabicyclooctane-class β-lactamase inhibitor designed to restore and enhance activity against extended-spectrum β-lactamase (ESBL) and some carbapenem-resistant Gram-negative pathogens. Piperacillin inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins and blocking the final transpeptidation step, leading to cell lysis, while enmetazobactam inhibits serine β-lactamases (including many ESBLs) that would otherwise hydrolyze piperacillin, thereby extending its spectrum and potency against resistant Enterobacterales and other Gram-negative organisms. The combination is being developed primarily for the treatment of serious infections such as complicated urinary tract infections and other multidrug-resistant Gram-negative infections.