Gepotidacin
Chemical compound
- None
- 1075236-89-3
Y
- 34982930
- DVF0PR037D
- D10878
- Interactive image
- c1cc(=O)n2c3c1ncc(=O)n3[C@@H](C2)CN4CCC(CC4)NCc5cc6c(cn5)OCCC6
InChI
- InChI=1S/C24H28N6O3/c31-22-4-3-20-24-29(22)15-19(30(24)23(32)13-27-20)14-28-7-5-17(6-8-28)25-11-18-10-16-2-1-9-33-21(16)12-26-18/h3-4,10,12-13,17,19,25H,1-2,5-9,11,14-15H2/t19-/m1/s1
- Key:PZFAZQUREQIODZ-LJQANCHMSA-N
Gepotidacin (INN[1]) is an experimental antibiotic that acts as a topoisomerase type II inhibitor.[2] It is being studied for the treatment of uncomplicated urinary tract infection (acute cystitis)[3] and infection with Neisseria gonorrhoeae (gonorrhea), including multidrug resistant strains.[4][5]
References
- ^ "International Nonproprietary Names for Pharmaceutical Substances" (PDF). WHO Drug Information. 28 (4). 2014.
- ^ Biedenbach DJ, Bouchillon SK, Hackel M, Miller LA, Scangarella-Oman NE, Jakielaszek C, et al. (January 2016). "In Vitro Activity of Gepotidacin, a Novel Triazaacenaphthylene Bacterial Topoisomerase Inhibitor, against a Broad Spectrum of Bacterial Pathogens". Antimicrobial Agents and Chemotherapy. 60 (3): 1918–1923. doi:10.1128/aac.02820-15. PMC 4776004. PMID 26729499.
- ^ Wagenlehner F, Perry CR, Hooton TM, Scangarella-Oman NE, Millns H, Powell M, et al. (February 2024). "Oral gepotidacin versus nitrofurantoin in patients with uncomplicated urinary tract infection (EAGLE-2 and EAGLE-3): two randomised, controlled, double-blind, double-dummy, phase 3, non-inferiority trials". Lancet. 403 (10428): 741–755. doi:10.1016/S0140-6736(23)02196-7. PMID 38342126. S2CID 267548740.
- ^ Scangarella-Oman NE, Hossain M, Dixon PB, Ingraham K, Min S, Tiffany CA, et al. (December 2018). "Microbiological Analysis from a Phase 2 Randomized Study in Adults Evaluating Single Oral Doses of Gepotidacin in the Treatment of Uncomplicated Urogenital Gonorrhea Caused by Neisseria gonorrhoeae". Antimicrobial Agents and Chemotherapy. 62 (12). doi:10.1128/AAC.01221-18. PMC 6256812. PMID 30249694.
- ^ Jacobsson S, Golparian D, Scangarella-Oman N, Unemo M (August 2018). "In vitro activity of the novel triazaacenaphthylene gepotidacin (GSK2140944) against MDR Neisseria gonorrhoeae". The Journal of Antimicrobial Chemotherapy. 73 (8): 2072–2077. doi:10.1093/jac/dky162. PMC 6927889. PMID 29796611.
- v
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(inhibit bacterial
purine metabolism,
thereby inhibiting
DNA and RNA
synthesis)
| DHFR inhibitor | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Sulfonamides (DHPS inhibitor) |
| ||||||||
| Combinations |
| ||||||||
| Other DHPS inhibitors |
(inhibit bacterial
topoisomerase
and/or DNA gyrase,
thereby inhibiting
DNA replication)
| 1st generation | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Fluoroquinolones |
| ||||||||
| Newer non-fluorinated | |||||||||
| Related (DG) |
inhibitors
| Nitroimidazole derivatives | |
|---|---|
| Nitrofuran derivatives |
| Rifamycins/ RNA polymerase | |
|---|---|
| Lipiarmycins |
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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