Gepotidacin Explained

Atc Prefix:None
Cas Number:1075236-89-3
Unii:DVF0PR037D
Chemspiderid:34982930
Kegg:D10878
Synonyms:GSK2140944
C:24
H:28
N:6
O:3
Smiles:c1cc(=O)n2c3c1ncc(=O)n3[C@@H](C2)CN4CCC(CC4)NCc5cc6c(cn5)OCCC6
Stdinchi: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
Stdinchikey: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]

Notes and References

  1. International Nonproprietary Names for Pharmaceutical Substances . WHO Drug Information . 28 . 4 . 2014.
  2. Biedenbach DJ, Bouchillon SK, Hackel M, Miller LA, Scangarella-Oman NE, Jakielaszek C, Sahm DF . 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 . January 2016 . 26729499 . 4776004 . 10.1128/aac.02820-15 .
  3. Wagenlehner F, Perry CR, Hooton TM, Scangarella-Oman NE, Millns H, Powell M, Jarvis E, Dennison J, Sheets A, Butler D, Breton J, Janmohamed S . 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 . February 2024 . 38342126 . 10.1016/S0140-6736(23)02196-7 . 267548740 .
  4. Scangarella-Oman NE, Hossain M, Dixon PB, Ingraham K, Min S, Tiffany CA, Perry CR, Raychaudhuri A, Dumont EF, Huang J, Hook EW, Miller LA . 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 . December 2018 . 30249694 . 6256812 . 10.1128/AAC.01221-18 .
  5. Jacobsson S, Golparian D, Scangarella-Oman N, Unemo M . In vitro activity of the novel triazaacenaphthylene gepotidacin (GSK2140944) against MDR Neisseria gonorrhoeae . The Journal of Antimicrobial Chemotherapy . 73 . 8 . 2072–2077 . August 2018 . 29796611 . 6927889 . 10.1093/jac/dky162 . free .