molecules of the month


oral prodrug of serine _-lactamase inh.

in dev. for multidrug resistant bact. infection

from optimization of prior _-lactamase inh.

J. Med. Chem., Jul. 24, 2020

Entasis Therapeutics, Waltham, MA

Structure of orally available diazabicyclooctane inhibitor, ETX0282
1 min read

ETX0282 is an oral prodrug of a class A, C, and D serine β-lactamase inhibitor in clinical development for drug-resistant enterobacterial infections in combination with the beta-lactam drug cefpodoxime proxetil. Impressively ETX0282 had no observed adverse effect levels (NOAELs) of 500 mg/kg/day and 400 mg/kg/day in rat and dog, respectively, despite the reactive-looking nature of the strained bridged carbamate core and the monofluoroether. I was surprised by the chemical stability of the fluoroether moiety, which can be seen in the co-crystal structure.

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