ETX0282

ETX0282 is an orally bioavailable ester prodrug of the diazabicyclooctane (DBO) serine β-lactamase inhibitor ETX1317. It is being developed in combination with cefpodoxime proxetil as an oral therapy for complicated urinary tract infections and other infections caused by multidrug-resistant and carbapenem-resistant Enterobacterales. Upon oral administration, ETX0282 is rapidly converted to its active form, ETX1317, which inhibits class A, C, and D serine β-lactamases by forming a reversible covalent acyl-enzyme complex at the active site of these enzymes. This inhibition restores the activity of partner β-lactam antibiotics against resistant bacteria. The drug was developed by Entasis Therapeutics[1][3][4][5][6][7].