ETTX - Entasis Therapeutics introduces ETX0462 targeting gram-negative and biothreat pathogens

Entasis Therapeutics Holdings (ETTX) presents preclinical data on ETX0462, a novel diazabicyclooctane with antimicrobial activity against multidrug-resistant ((MDR)) Gram-negative and biothreat pathogens, at the 2021 World Microbe Forum. Entasis scientists further demonstrated that the activity of ETX0462 was unaffected by all four Ambler classes of ?-lactamases and has a low propensity for resistance emergence due to its ability to permeate bacterial cells through multiple porins and inhibit several PBPs. In in vivo studies, ETX0462 exhibited robust bactericidal activity reaching >3-log drop in bacterial count vs. initial inoculum in a neutropenic murine lung model against clinical isolates of P. aeruginosa.Similar in vivo efficacy was also demonstrated for the biothreat pathogens Y. pestis and B. pseudomallei.Entasis demonstrated that ETX0462 was well tolerated in a rat 14-day GLP toxicology study reaching the limit dose of 2,000 mg/kg.

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Entasis Therapeutics introduces ETX0462 targeting gram-negative and biothreat pathogens