ETX-0282 CPDP

ETX-0282 CPDP is an oral combination of ETX-0282, a prodrug that is hydrolyzed in vivo to ETX1317, a diazabicyclooctane β-lactamase inhibitor, with cefpodoxime proxetil (CPDP), an oral prodrug of the cephalosporin cefpodoxime. ETX1317 inhibits Ambler class A and C β-lactamases and select class D enzymes, restoring cefpodoxime activity against multidrug-resistant Enterobacteriaceae including ESBL- and some carbapenemase-producers; it does not inhibit class B metallo-β-lactamases. The combo is being developed as an oral therapy for complicated urinary tract infections and other MDR Gram-negative infections. Phase 1 studies in healthy volunteers evaluated safety, tolerability, and pharmacokinetics of ETX-0282 alone and combined with CPDP, with initial results reported by Entasis Therapeutics. Preclinical PK/PD and murine thigh infection models demonstrated that oral ETX-0282 plus CPDP reduces bacterial burden when unbound exposures meet target thresholds, with high bioavailability and near-complete conversion of ETX-0282 to ETX1317 across species supporting fixed oral dosing with CPDP.[2][4][7][3][5][1]

Brand names

ETX0282CPDPETX-0282CPDPETX 0282CPDP

Other names

ETX0282CPDPETX-0282CPDPETX 0282CPDPETX0282 + cefpodoxime proxetilCPDP-ETX0282CPDP-ETX-0282CPDP-ETX 0282