Zoliflodacin

Zoliflodacin (development codes AZD0914 and ETX0914) is an experimental antibiotic that is being studied for the treatment of infection with Neisseria gonorrhoeae (gonorrhea).[1] It has a novel mechanism of action which involves inhibition of bacterial type II topoisomerases.[2] It is being developed by Entasis Therapeutics and is (as of 2020) in Phase III clinical trials.[3]

Zoliflodacin
Clinical data
Other namesAZD0914; ETX0914
Pregnancy
category
  • Not classified yet
Routes of
administration		Oral
Drug classAntibiotic
Legal status
Legal status
Pharmacokinetic data
Bioavailability97.8%
MetabolismHepatic
Onset of action
  • Fasted: 1.5–2.3 h
  • Fed: 4 h
Elimination half-life5.3–6.3 h
Excretion
Identifiers
CAS Number
PubChem CID
DrugBank
UNII
KEGG
Chemical and physical data
FormulaC22H22FN5O7
Molar mass487.444 g·mol−1
3D model (JSmol)
  • C[C@@H]1CN2[C@H]([C@@H](O1)C)C3(CC4=C2C(=C5C(=C4)C(=NO5)N6[C@H](COC6=O)C)F)C(=O)NC(=O)NC3=O
  • InChI=1S/C22H22FN5O7/c1-8-7-33-21(32)28(8)17-12-4-11-5-22(18(29)24-20(31)25-19(22)30)16-10(3)34-9(2)6-27(16)14(11)13(23)15(12)35-26-17/h4,8-10,16H,5-7H2,1-3H3,(H2,24,25,29,30,31)/t8-,9+,10-,16+/m0/s1
  • Key:ZSWMIFNWDQEXDT-ZESJGQACSA-N

References
  1. Taylor SN, Marrazzo J, Batteiger BE, Hook EW, Seña AC, Long J, et al. (November 2018). "Single-Dose Zoliflodacin (ETX0914) for Treatment of Urogenital Gonorrhea". The New England Journal of Medicine. 379 (19): 1835–1845. doi:10.1056/NEJMoa1706988. hdl:1805/19865. PMID 30403954.
  2. Basarab GS, Kern GH, McNulty J, Mueller JP, Lawrence K, Vishwanathan K, et al. (July 2015). "Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases". Scientific Reports. 5: 11827. Bibcode:2015NatSR...511827B. doi:10.1038/srep11827. PMC 4501059. PMID 26168713.
  3. "Pipeline". Entasis Therapeutics.
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