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IS-159, also known as serotonin-O-carboxymethylglycyltyrosinamide, is a triptan-like serotonin 5-HT1B and 5-HT1D receptor agonist which was under development for the treatment of migraine but was never marketed.[1][2][3][6][5][7] It is taken intranasally or subcutaneously.[1][2][3]

The drug is a small serotonin-containing peptide and is described as being peripherally selective.[3] It acts as a selective and potent serotonin 5-HT1B and 5-HT1D receptor agonist (Ki = 3.2 nM and 1.6 nM, respectively).[8][4] IS-159 has more than 300-fold lower affinity for the serotonin 5-HT1A receptor (Ki = 1,000) and is inactive at the serotonin 5-HT1E and 5-HT1F receptors (Ki = >10,000 nM).[8][9][10] The drug’s pharmacokinetics in humans have been studied.[2][4][5]

IS-159 was originated by Immunotech in France and was under development by Immunotech and The Medicines Company in the 1990s and early 2000s, but development was discontinued in 2003.[1][2] The drug reached phase 2 clinical trials prior to the discontinuation of its development.[1][2][5]

See also

References

  1. ^ a b c d e “IS 159”. AdisInsight. 17 January 2020. Retrieved 25 January 2026.
  2. ^ a b c d e f g h “IS 159”. Drugs in R&D. 2 (6): 390–391. December 1999. doi:10.2165/00126839-199902060-00006. PMID 10763448.
  3. ^ a b c d Mucke H (December 2002). “Therapies in development for the treatment of migraine”. Expert Opinion on Investigational Drugs. 11 (12): 1813–1820. doi:10.1517/13543784.11.12.1813. PMID 12457440.
  4. ^ a b c d Ramadan NM (2001). “Acute treatments: future developments”. Current Medical Research and Opinion. 17 Suppl 1: s81–s86. doi:10.1185/0300799039117018. PMID 12463284.
  5. ^ a b c d Dingemanse J, Soubrouillard C, Paris J, Pisano P, Blin O (August 2000). “Pronounced effect of caprylocaproyl macrogolglycerides on nasal absorption of IS-159, a peptide serotonin 1B/1D-receptor agonist”. Clinical Pharmacology and Therapeutics. 68 (2): 114–121. doi:10.1067/mcp.2000.108196. PMID 10976542.
  6. ^ Ramadan NM, Buchanan TM, Pearlman SH (2004). “Clinical Science: Peripheral and Central Trigeminal Targets for Acute Migraine Therapy: Early Clinical Trial Results”. Headache Currents. 1 (1): 7–12. doi:10.1111/j.1743-5013.2004.10104.x. ISSN 1743-5005. Retrieved 25 January 2026.
  7. ^ Chauveau J, Delaage MA (1997). “IS-159: A High-Affinity Specific 5-HT1D Full Receptor Agonist, Effective in the Acute Treatment of Migraine”. Frontiers in Headache Research. 6th International Headache Research Seminar; 1995 Nov 17-19. 6. Copenhagen: 287–292.
  8. ^ a b Martin GR (1997). “Serotonin Receptor Involvement in the Pathogenesis and Treatment of Migraine”. In Goadsby VG, Silberstein SD (eds.). Blue Books of Practical Neurology. Vol. 17. pp. 25–38. ISBN 978-0-7506-9871-9.
  9. ^ Waeber C (November 2003). “Emerging drugs in migraine treatment”. Expert Opinion on Emerging Drugs. 8 (2): 437–456. doi:10.1517/14728214.8.2.437. PMID 14661998.
  10. ^ van den Broek RW (13 March 2002). Vascular Effects of Antimigraine Drugs: pharmacology of human in vitro models in migraine. RePub, Erasmus University Repository (Doctoral thesis). Erasmus University Rotterdam. Retrieved 25 January 2026.