Bacterial resistance to leucyl-tRNA synthetase inhibitor GSK2251052 develops during treatment of complicated urinary tract infections.

doi:10.1128/AAC.03774-14

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Bacterial resistance to leucyl-tRNA synthetase inhibitor GSK2251052 develops during treatment of complicated urinary tract infections.

Antimicrobial agents and chemotherapy - 1 Jan 2015

O'Dwyer Karen, Spivak Aaron T, Ingraham Karen, Min Sharon, Holmes David J, Jakielaszek Charles, Rittenhouse Stephen, Kwan Alan L, Livi George P, Sathe Ganesh, Thomas Elizabeth, Van Horn Stephanie, Miller Linda A, Twynholm Monique, Tomayko John, Dalessandro Marybeth, Caltabiano Madelyn, Scangarella-Oman Nicole E, Brown James R

Abstract excerpt

GSK2251052, a novel leucyl-tRNA synthetase (LeuRS) inhibitor, was in development for the treatment of infections caused by multidrug-resistant Gram-negative pathogens. In a phase II study (study LRS114688) evaluating the efficacy of GSK2251052 in complicated urinary tract infections, resistance developed very rapidly in 3 of 14 subjects enrolled, with ≥32-fold increases in the GSK2251052 MIC of the infecting...

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PMID: 25348524
DOI: 10.1128/AAC.03774-14
PMCID: PMC4291364

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