ArticleAntimicrobial agents and chemotherapy2015
Pharmacodynamic Profile of GSK2140944 against Methicillin-Resistant Staphylococcus aureus in a Murine Lung Infection Model.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Novel Bacterial Topoisomerase Inhibitors: A New Front in an Old War.Journal of molecular biology · 2026Review
- Simulating treatment effects for gonorrhoea using a within-host mathematical model.Infectious Disease Modelling · 2026Article
- Efficacy of therapeutically administered gepotidacin in a rabbit model of inhalational anthrax.Antimicrobial agents and chemotherapy · 2024Article
- Efficacy of Intravenously Administered Gepotidacin in Cynomolgus Macaques following a Francisella tularensis Inhalational Challenge.Antimicrobial agents and chemotherapy · 2023Article
- Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 1.RSC medicinal chemistry · 2020Article
- Pharmacokinetics and Pharmacodynamics of Gamithromycin Treatment ofFrontiers in pharmacology · 2019Article
- Cellular Pharmacokinetics and Intracellular Activity of Gepotidacin against Staphylococcus aureus Isolates with Different Resistance Phenotypes in Models of Cultured Phagocytic Cells.Antimicrobial agents and chemotherapy · 2018Article
- What we may expect from novel antibacterial agents in the pipeline with respect to resistance and pharmacodynamic principles.Journal of pharmacokinetics and pharmacodynamics · 2017Review
- Antibiotics in the clinical pipeline at the end of 2015.The Journal of antibiotics · 2017Review
- Multicenter Investigation of Gepotidacin (GSK2140944) Agar Dilution Quality Control Determinations for Neisseria gonorrhoeae ATCC 49226.Antimicrobial agents and chemotherapy · 2016Article
- In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens.Antimicrobial agents and chemotherapy · 2016Article
- Investigational drugs to treat methicillin-resistant Staphylococcus aureus.Expert opinion on investigational drugs · 2016Review
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Authors and funding
3 authors.
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Abstract
GSK2140944 is a novel bacterial type II topoisomerase inhibitor with in vitro activity against key causative respiratory pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). We described the pharmacodynamics of GSK2140944 against MRSA in the neutropenic murine lung infection model. MICs of GSK2140944 were determined by broth microdilution. Plasma and epithelial lining fluid (ELF) pharmacokinetics were evaluated to allow determination of pulmonary distribution. Six MRSA isolates were tested. GSK2140944 doses of 1.56 to 400 mg/kg of body weight every 6 h (q6h) were utilized. Efficacy as the change in log10 CFU at 24 h compared with 0 h controls and the area under the concentration-time curve for the free, unbound fraction of a drug (fAUC)/MIC required for various efficacy endpoints were determined. GSK2140944 MICs were 0.125 to 0.5 mg/liter against the six MRSA isolates. ELF penetration ratios ranged from 1.1 to 1.4. Observed maximal decreases were 1.1 to 3.1 log10 CFU in neutropenic mice. The mean fAUC/MIC ratios required for stasis and 1-log-unit decreases were 59.3 ± 34.6 and 148.4 ± 83.3, respectively. GSK2140944 displayed in vitro and in vivo activity against MRSA. The pharmacodynamic profile of GSK2140944, as determined, supports its further development as a potential treatment option for pulmonary infections, including those caused by MRSA.
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