Chemistry:IS-159

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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][4][5][6] 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).[7][8] 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).[7][9][10] The drug's pharmacokinetics in humans have been studied.[2][8][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. ↑ 1.0 1.1 1.2 1.3 "IS 159". 17 January 2020. https://adisinsight.springer.com/drugs/800005786. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 "IS 159". Drugs in R&D 2 (6): 390–391. December 1999. doi:10.2165/00126839-199902060-00006. PMID 10763448. 
  3. ↑ 3.0 3.1 3.2 "Therapies in development for the treatment of migraine". Expert Opinion on Investigational Drugs 11 (12): 1813–1820. December 2002. doi:10.1517/13543784.11.12.1813. PMID 12457440. 
  4. ↑ "Clinical Science: Peripheral and Central Trigeminal Targets for Acute Migraine Therapy: Early Clinical Trial Results". Headache Currents 1 (1): 7–12. 2004. doi:10.1111/j.1743-5013.2004.10104.x. ISSN 1743-5005. https://headachejournal.onlinelibrary.wiley.com/doi/10.1111/j.1743-5013.2004.10104.x. Retrieved 25 January 2026. 
  5. ↑ 5.0 5.1 5.2 "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. August 2000. doi:10.1067/mcp.2000.108196. PMID 10976542. 
  6. ↑ "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 (Copenhagen) 6: 287–292. 1997. https://scholar.google.com/scholar?cluster=11574284863240451397. 
  7. ↑ 7.0 7.1 "Serotonin Receptor Involvement in the Pathogenesis and Treatment of Migraine". Blue Books of Practical Neurology. 17. 1997. pp. 25–38. ISBN 978-0-7506-9871-9. https://archive.org/details/headache0000unse/page/32/. 
  8. ↑ 8.0 8.1 "Acute treatments: future developments". Current Medical Research and Opinion 17 Suppl 1: s81–s86. 2001. doi:10.1185/0300799039117018. PMID 12463284. 
  9. ↑ "Emerging drugs in migraine treatment". Expert Opinion on Emerging Drugs 8 (2): 437–456. November 2003. 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.



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