AAI-101

Research use only, not for human use.

AAI-101 is a novel extended-spectrum β-lactamase inhibitor with activity against many β-lactamases, including some class A and class D carbapenemases.

AAI-101 is a novel extended-spectrum β-lactamase inhibitor with activity against many β-lactamases, including some class A and class D carbapenemases; is currently in clinical development as a combination with cefepime, reduces the MIC50 of cefepime against a collection of 223 cefepime-nonsusceptible isolates of the family Enterobacteriaceae from >64 mg/L to 0.125 mg/L.Bacterial Infection Phase 1 Clinical(In Vitro):Enmetazobactam shows potent activity against specific resistance phenotypes with MIC50 and MIC90 of 0.125 mg/L and 64 mg/L. 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. (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.

Enmetazobactam shows potent activity against specific resistance phenotypes with MIC50 and MIC90 of 0.125 mg/L and 64 mg/L. 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.

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.

AAI 101 | AAI101

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

1001404-83-6

314.32

C11H14N4O5S

>98% (HPLC)

DMSO : ≥ 113.3 mg/mL 360.46 mM

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

(2S,3S,5R)-3-methyl-3-((1-methyl-1H-1,2,3-triazol-3-ium-3-yl)methyl)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate 4,4-dioxide

(-20℃)

With Ice Pack

≥ 2 years