Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor. Zoliflodacin has potent in vitro antibacterial activity against Gram-positive and Gram-negative organisms, including S. aureus with the MIC90 of 0.25 μg/mL.
1.Basarab GS, Kern GH, McNulty J, Mueller JP, Lawrence K, Vishwanathan K, Alm RA, Barvian K, Doig P, Galullo V et al.. (2015) Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases.. Sci Rep, 5 (13):(11827). [PMID:26168713][10.1021/op500134e]
2.Bradford PA, Miller AA, O'Donnell J, Mueller JP. (2020) Zoliflodacin: An Oral Spiropyrimidinetrione Antibiotic for the Treatment of Neisseria gonorrheae, Including Multi-Drug-Resistant Isolates.. ACS Infect Dis, 6 (6):(1332-1345). [PMID:32329999][10.1021/op500134e]
3.Luckey A, Alirol E, Delhomme S, O'Donnell J, Bettiol E, Mueller J, O'Brien S, Gillon JY. (2023) Effect of food on the pharmacokinetics of zoliflodacin granules for oral suspension: Phase I open-label randomized cross-over study in healthy subjects.. Clin Transl Sci, 71 (13):(1755-70). [PMID:36824016][10.1021/op500134e]
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