Enmetazobactam  (Synonyms: AAI101)

Enmetazobactam (AAI101) is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

314.32

Solid

C₁₁H₁₄N₄O₅S

1001404-83-6

C[N+]1=NN(C[C@@](S([C@]2([H])C3)(=O)=O)(C)[C@H](C([O-])=O)N2C3=O)C=C1

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Crandon JL, et al. In Vitro Activity of Cefepime/AAI101 and Comparators against Cefepime Non-susceptible Enterobacteriaceae. Pathogens. 2015 Aug 18;4(3):620-5.  [Content Brief]

  [2]. Crandon JL, et al. In vivo activities of simulated human doses of cefepime and cefepime-AAI101 against multidrug-resistant Gram-negative Enterobacteriaceae. Antimicrob Agents Chemother. 2015 May;59(5):2688-94.  [Content Brief]