Antibiotic resistance – or antimicrobial resistance (AMR) – has been making headlines for decades. At TAXIS Pharmaceuticals, we have been working since 2009 on the development of compounds that combat antimicrobial resistance.
Efflux pumps in Gram-negative bacteria such as Pseudomonas aeruginosa provide intrinsic antimicrobial resistance by facilitating the extrusion of a wide range of antimicrobials. Approaches for combating efflux-mediated multidrug resistance involve, in part, developing indirect antimicrobial agents capable of inhibiting efflux, thus rescuing the activity of antimicrobials previously rendered inactive by efflux. Herein, TXA09155 is presented as a novel efflux pump inhibitor (EPI) formed by conformationally constraining our previously reported EPI TXA01182. TXA09155 demonstrates strong potentiation in combination with multiple antibiotics with efflux liabilities against wild-type and multidrug-resistant (MDR) P. aeruginosa.
Efflux Pump Inhibitor (EPI) drug candidates appears in the August 13th special Antibiotic Alternatives issue of ACS Infectious Diseases. The paper titled “The CARB-X Portfolio of Nontraditional Antibacterial Products”