Gepotidacin

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]

Gepotidacin
Clinical data
Other namesGSK2140944
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
ChemSpider
UNII
KEGG
ECHA InfoCard100.249.088
Chemical and physical data
FormulaC24H28N6O3
Molar mass448.527 g·mol−1
3D model (JSmol)
SMILES
  • 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

References
  1. "International Nonproprietary Names for Pharmaceutical Substances" (PDF). WHO Drug Information. 28 (4). 2014.
  2. Biedenbach DJ, Bouchillon SK, Hackel M, Miller LA, Scangarella-Oman NE, Jakielaszek C, Sahm DF (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): 1918–23. doi:10.1128/aac.02820-15. PMC 4776004. PMID 26729499.
  3. "GlaxoSmithKline kick-starts first-of-its-kind late-stage antibiotic test". FierceBiotech. Retrieved 29 October 2019.
  4. 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.
  5. 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.
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