Entasis Therapeutics Introduces ETX0462, a First-in-Class Candidate, Targeting Multidrug-Resistant Gram-Negative and Biothreat Pathogens
“ETX0462 is the latest product candidate to emerge from our discovery platform and the first example of a novel class of agents targeting the established mechanism of β-lactam antibiotics without being susceptible to the most common β-lactam resistance mechanism, β-lactamases,” commented
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 also shared that the PK/PD index of ETX0462 is driven by % Time > MIC and a ~60% target for 1-log bactericidal activity. Entasis demonstrated that ETX0462 was well tolerated in a rat 14-day GLP toxicology study reaching the limit dose of 2,000 mg/kg.
Additional details of the ETX0462 data presented can be found on the Entasis Presentations webpage.
Entasis is a clinical-stage biopharmaceutical company focused on the discovery, development and commercialization of novel antibacterial products to treat serious infections caused by multidrug-resistant Gram-negative bacteria. Entasis’ pathogen-targeted design platform has produced a pipeline of product candidates, including SUL-DUR (targeting Acinetobacter baumannii infections), zoliflodacin (targeting Neisseria gonorrhoeae infections), ETX0282CPDP (targeting Enterobacterales infections) and ETX0462 (targeting Pseudomonas infections). For more information, visit www.entasistx.com.
ETX0462 is a novel, first-in-class, diazabicyclooctane with antimicrobial activity against multidrug-resistant (MDR) Gram-negative and biothreat pathogens including, P. aeruginosa, K. pneumoniae, S. maltophilia, E. coli, B. anthracis, Y. pestis, F. tularensis and Burkholderia spp. Similar to β-lactam antibiotics, ETX0462 inhibits penicillin-binding proteins which are essential for bacterial cell wall biosynthesis, however, unlike β-lactam antibiotics, ETX0462 is unaffected by β-lactamase mediated resistance. ETX0462 is supported by CARB-X.
|Company Contact||Investor Contact|
|(781) 810-0114||(929) 469-3859|
Source: Entasis Therapeutics Holdings Inc.