Cligosiban

Last updated

Cligosiban
Cligosiban.svg
Clinical data
Other namesIX-01; IX01; PF-3274167; PF3274167; PF-03274167; PF03274167; PF-327,4167
Routes of
administration 		Oral [1] [2]
Drug class Oxytocin receptor antagonist
Pharmacokinetic data
Elimination half-life 12 hours [3]
Identifiers
  • 5-[3-[3-(2-chloro-4-fluorophenoxy)azetidin-1-yl]-5-(methoxymethyl)-1,2,4-triazol-4-yl]-2-methoxypyridine
CAS Number
PubChem CID
DrugBank
UNII
ChEMBL
Chemical and physical data
Formula C19H19ClFN5O3
Molar mass 419.84 g·mol−1
3D model (JSmol)
  • COCC1=NN=C(N1C2=CN=C(C=C2)OC)N3CC(C3)OC4=C(C=C(C=C4)F)Cl
  • InChI=1S/C19H19ClFN5O3/c1-27-11-17-23-24-19(26(17)13-4-6-18(28-2)22-8-13)25-9-14(10-25)29-16-5-3-12(21)7-15(16)20/h3-8,14H,9-11H2,1-2H3
  • Key:HNIFCPBQMKPRCX-UHFFFAOYSA-N

Cligosiban (INN Tooltip International Nonproprietary Name; developmental code names IX-01 and PF-3274167) is an oxytocin receptor antagonist which is or was under development for the treatment of premature ejaculation. [1] [4] [5] [2] [3] It is taken orally. [1] [2] The drug is a small molecule or non-peptide and is a potent, highly selective, and brain-penetrant antagonist of the oxytocin receptor. [5] [2] Cligosiban was originated by Pfizer and is under development by Ixchelsis and Chorus Group. [1] [4] As of December 2019, it is in phase 2 clinical trials. [1] However, another source lists the drug's development as having been discontinued. [4] The drug failed to show effectiveness in a phase 2b trial. [6]

See also

References

  1. 1 2 3 4 5 "Cligosiban". AdisInsight. 28 December 2019. Retrieved 27 January 2026.
  2. 1 2 3 4 Osterloh IH, Muirhead GJ, Sultana S, Whaley S, van den Berg F, Atiee G (November 2018). "Pharmacokinetics, Safety, and Tolerability of Single Oral Doses of a Novel Oxytocin Receptor Antagonist-Cligosiban-in Development for Premature Ejaculation: Three Randomized Clinical Trials in Healthy Subjects". The Journal of Sexual Medicine. 15 (11): 1547–1557. doi:10.1016/j.jsxm.2018.09.006. PMID   30341006.
  3. 1 2 Muirhead GJ, Osterloh IH, Whaley S, van den Berg F (February 2019). "Pharmacokinetics, Safety, and Tolerability of Multiple Doses of the Novel Oxytocin Receptor Antagonist Cligosiban in Development for Premature Ejaculation: Two Randomized Clinical Trials in Healthy Subjects". The Journal of Sexual Medicine. 16 (2): 213–222. doi:10.1016/j.jsxm.2018.11.012. PMID   30612858.
  4. 1 2 3 "Delving into the Latest Updates on Cligosiban with Synapse". Synapse. 17 January 2026. Retrieved 27 January 2026.
  5. 1 2 Wayman C, Russell R, Tang K, Weibly L, Gaboardi S, Fisher L, et al. (December 2018). "Cligosiban, A Novel Brain-Penetrant, Selective Oxytocin Receptor Antagonist, Inhibits Ejaculatory Physiology in Rodents". The Journal of Sexual Medicine. 15 (12): 1698–1706. doi:10.1016/j.jsxm.2018.10.008. PMID   30527053.
  6. ↑ Althof S, Osterloh IH, Muirhead GJ, George K, Girard N (August 2019). "The Oxytocin Antagonist Cligosiban Fails to Prolong Intravaginal Ejaculatory Latency in Men with Lifelong Premature Ejaculation: Results of a Randomized, Double-Blind, Placebo-Controlled Phase IIb trial (PEDRIX)". The Journal of Sexual Medicine. 16 (8): 1188–1198. doi:10.1016/j.jsxm.2019.05.015. PMID   31351660.
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