In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens

  • Antimicrob Agents Chemother. 2016 Jan 4;60(3):1918-23. doi: 10.1128/AAC.02820-15.
D J Biedenbach  1 ,  S K Bouchillon  2 ,  M Hackel  2 ,  L A Miller  3 ,  N E Scangarella-Oman  3 ,  C Jakielaszek  3 ,  D F Sahm  2
Affiliations
  • 1. International Health Management Associates, Inc., Schaumburg, Illinois, USA [email protected].
  • 2. International Health Management Associates, Inc., Schaumburg, Illinois, USA.
  • 3. GlaxoSmithKline, Collegeville, Pennsylvania, USA.
PMID: 26729499 DOI: 10.1128/AAC.02820-15
Abstract

Gepotidacin inhibits Bacterial DNA replication through a mode different from that of fluoroquinolones. Gepotidacin and comparators were tested by broth and agar dilution against clinical isolates. The in vitro activities of gepotidacin were comparable against methicillin-susceptible and -resistant Staphylococcus aureus (MSSA and MRSA, respectively) isolates (MIC90, 0.5 μg/ml). The gepotidacin MIC90s were as follows (in micrograms per milliliter) for the indicated bacteria: Streptococcus pyogenes, 0.25; Escherichia coli, 2; Moraxella catarrhalis, ≤ 0.06; Streptococcus pneumoniae (0.25), Haemophilus influenzae, 1; Clostridium perfringens, 0.5; and Shigella spp., 1, including levofloxacin-resistant subsets. Gepotidacin warrants further investigation for clinical development.

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