As a medicinal chemist who worked on the NBTI Antimicrobial Agents, I am really excited to see that GSK is still pushing a candidate forward for the treatment of conventional and biothreat pathogens, such as methicillin-resistant Staphylococcus aureus. Based on the pioneer works at GSK and Aventis in late 1990’s, the last fifteen years has witnessed extraordinary efforts from GSK, Aventis, Johnson and Johnson, Biovertis, AstraZeneca, Actelion, Toyama, Pfizer, Merck and Daiichi. There have accumulated well over 100 patents and patent applications. As many candidates failed to progress, the works out of a few hundred chemists worldwide are gradually getting to see the light. I hope that GSK2140944 will eventually make it, so that all our work will not be in vain! I draw a few representative structures to show the genuine creativity during these true international competitions. I also wish that the antibacterial world will see this kind of race again!
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October 28, 2020, GSK starts a phase III clinical programme for a potential first-in-class antibiotic, gepotidacin(GSK2140944) is the first in a new class of antibiotics, called triazaacenaphthylene topoisomerase inhibitors, developed at GSK in 2007 with a novel “dual targeting” mechanism of action (MOA) and oral formulation. Its MOA is distinct from any currently approved antibiotic. Fantastic news!
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