Gepotidacin is a novel triazaacenaphthylene inhibitor of bacterial type II topoisomerase.

Gepotidacin has in vitro activity against causative pathogens of acute bacterial skin and skin structure infections (ABSSSIs) [3]. Gepotidacin that inhibits bacterial DNA gyrase and topoisomerase IV via a unique mechanism and has demonstrated in vitro activity against gram-negative and gram-positive bacterias, including drug-resistant strains, and also targets pathogens associated with other conventional and biothreat infections. The MIC50 and MIC90 for gepotidacin against the 25 N. Gonorrhoeae isolate tested are 0.12 and 0.25 μg/mL, respectively [1]. The gepotidacin MIC90s are as follows: Streptococcus pyogenes (0.25 μg/mL); Escherichia coli (2 μg/mL); Moraxella catarrhalis (≤0.06 μg/mL); Streptococcus pneumoniae (0.25 μg/mL); Haemophilus influenzae (1 μg/mL); Clostridium perfringens (0.5 μg/mL); and Shigella spp. (1 μg/mL) [2].

ELF penetration ratios range from 1.1 to 1.4. GSK2140944 MICs are 0.125 to 0.5 mg/L against the six MRSA isolates. The mean of AUC/MIC ratios required for stasis and 1-log-unit decreases are 59.3 ± 34.6 and 148.4 ± 83.3, respectively. Observed maximal decreases are 1.1 to 3.1 log10 CFU in neutropenic mice [4].