GSK Submits Prospectus for Novel Antibiotic Gepotidacin (GSK2140944): A First-in-Class Dual-Targeting Oral Agent for uUTI and Gonorrhea

Drug Name:gepotidacin

CAS：1075236-89-3

R&D Code:GSK2140944

Original Research Company:GSK

2023Year4Month15Day,GSKPublishedgepotidacinThe KeyEAGLE-2AndEAGLE-3 IIIPositive results from the Phase clinical trial.

InEAGLE-2 IIIIn the trial period,gepotidacinIn50.6%in patients, showing a treatment success rate, whilenitrofurantoinFor47%. InEAGLE-3 IIIIn the trial period,gepotidacinIn58.5%in patients, showing a treatment success rate, whilenitrofurantoinFor43.6%. In two trials, as of the28Daily follow-up visit,94%AcceptgepotidacinThe patients were not given any additional treatment during the trial period.uUTIAntibiotic treatment. InEAGLE-2AndEAGLE-3 IIIIn the trial period,gepotidacinThe safety and tolerability ofgepotidacinConsistent test results.

[i]Difference:gepotidacin - nitrofurantoin。Micro-ITT NTF-S (IAGroup), Microbial Intention-to-Treat Nitrofurantoin-Sensitive Population Interim Analysis Group

[ii]Composite Endpoint of Clinical and Microbiological Success

[iii]Clinical Cure Trial Successful(TOC) =Symptom Resolution

[iv]Eligible urinary pathogens eradicated to103 CFU/mL

2024Year2Month26Day,GSKAnnouncementgepotidacinCriticalEAGLE-1 IIIPositive Top-Line Results Achieved in the Phase Trial.The trial met its primary efficacy endpoint,gepotidacin(Oral, two doses,3000Milligram)Compared with intramuscular injection(IM)Ceftriaxone(500Milligram)Add oral azithromycin(1000Milligram)In comparison, it demonstrated non-inferiority. The results are based on post-treatment.3-7Day's Treatment Trial(ToC)Access to the primary endpoint of the microbial response.

GepotidacinIt is a new type of antibacterial drug that inhibits bacteria through a novel mechanism of action and binding site.DNAReplication provides two different types for most pathogens.IIBalanced inhibition of type topoisomerase.

This provides activity against most target urinary tract pathogens and strains of Neisseria gonorrhoeae, including isolates resistant to existing antibiotics. Due to the well-balanced inhibition of both enzymes, targeted mutations in both are required to significantly affectgepotidacinSusceptibility.

References:WO2008128942,WO2004058144