molecules of the month


oral BID antibacterial Type II topoisomerase inhibitor

Ph. III for uncomplicated UTIs

from unbiased antibacterial screen + opt.

ECCMID, April 2023

Glaxo (GSK), Stevenage, UK

gepotidacin, bacterial topoisomerase, oral BID antibacterial, Type II topoisomerase inhibitor, Ph. III for uncomplicated UTIs, from unbiased antibacterial screen + opt., ECCMID, April 2023, GLAXO (GSK), STEVENAGE, UK
5 mins read

A potential first-in-class oral antibiotic with recent positive Ph. III data. The orally administered gepotidacin is a member of a novel class of type IIA topoisomerase inhibitors, also called novel bacterial topoisomerase inhibitors (NBTIs), for which the mode of action and binding mode with a topoisomerase was first disclosed in 2010 by GSK. NBTIs target the bacterial type IIA topoisomerase enzymes DNA gyrase and DNA topoisomerase IV, which are A2B2 tetramers that cleave and reseal DNA to change its topology. While these are also the targets of the more established fluoroquinolone class of antibiotics that are now experiencing issues with bacterial resistance (e.g. ciprofloxacin, levofloxacin and moxifloxacin), the distinct binding mode and mechanism of action of gepotidacin can help it…

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