Enmetazobactam

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens^[1][2]. In Vitro:Enmetazobactam shows potent activity against specific resistance phenotypes with MIC₅₀ and MIC₉₀ of 0.125 mg/L and 64 mg/L^[1]. Cefepime-Enmetazobactam MICs decreases with increasing concentrations of Enmetazobactam (over the range from 1 to 16 mg/L) for most strains, demonstrating a concentration dependence of Enmetazobactam on restoration of the antibacterial activity of the cephalosporin^[1]. In Vivo:In neutropenic animals, cefepime-Enmetazobactam treatment results in reductions in bacterial density of ≥0.5 log₁₀ CFU for 12 of the 20 strains tested and reductions of ≥1 log₁₀ CFU for 6 of these. Increases in bacterial density are for only four strains, three of which have cefepime-Enmetazobactam MICs of ≥64 mg/L, irrespective of the Enmetazobactam concentration^[2].