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IS-159

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IS-159
Clinical data
Other namesIS159; Serotonin-O-carboxymethylglycyltyrosinamide; Serotonin-carboxylmethyleneoxy-L-tyrosylglycinamide; 2-(3-(2-aminoethyl)-1H-indol-5-yloxy)acetyl-L-tyrosyl-glycinamide
Routes of
administration		Intranasal, subcutaneous[1][2][3]
Drug classSerotonin 5-HT1B and 5-HT1D receptor agonist; Triptan-like drug; Antimigraine agent
ATC code
  • None
Pharmacokinetic data
Onset of action15–20 minutes (TmaxTooltip time to peak levels)[2][4]
Elimination half-life2–2.5 hours[2][4][5]
Identifiers
  • (2S)-2-[[2-[[3-(2-aminoethyl)-1H-indol-5-yl]oxy]acetyl]amino]-N-(2-amino-2-oxoethyl)-3-(4-hydroxyphenyl)propanamide
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC23H27N5O5
Molar mass453.499 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1C[C@@H](C(=O)NCC(=O)N)NC(=O)COC2=CC3=C(C=C2)NC=C3CCN)O
  • InChI=1S/C23H27N5O5/c24-8-7-15-11-26-19-6-5-17(10-18(15)19)33-13-22(31)28-20(23(32)27-12-21(25)30)9-14-1-3-16(29)4-2-14/h1-6,10-11,20,26,29H,7-9,12-13,24H2,(H2,25,30)(H,27,32)(H,28,31)/t20-/m0/s1
  • Key:PBRWGFLPYQYNGI-FQEVSTJZSA-N

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 (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

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References

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  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 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 Opin Investig 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". Curr Med Res Opin. 17 Suppl 1: s81–6. 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". Clin Pharmacol Ther. 68 (2): 114–121. doi:10.1067/mcp.2000.108196. PMID 10976542.
  6. ^ Ramadan, Nabih M.; Buchanan, Thomas M.; Pearlman, Starr H. (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, M. A. (1997). IS-159: A High-Affinity Specific 5-HT1D Full Receptor Agonist, Effective in the Acute Treatment of Migraine. Frontiers in Headache Research, 6, 287–292. / 6th International Headache Research Seminar; 1995 Nov 17-19; Copenhagen, 57. https://scholar.google.com/scholar?cluster=11574284863240451397
  8. ^ a b Martin, G. R. (1997). Serotonin receptor involvement in the pathogenesis and treatment of migraine. BLue Books of Practical Neurology, 17, 25–38. https://archive.org/details/headache0000unse/page/32/
  9. ^ Waeber C (November 2003). "Emerging drugs in migraine treatment". Expert Opin Emerg Drugs. 8 (2): 437–456. doi:10.1517/14728214.8.2.437. PMID 14661998.
  10. ^ Broek, van den (13 March 2002). "Vascular Effects of Antimigraine Drugs: pharmacology of human in vitro models in migraine". RePub, Erasmus University Repository. Retrieved 25 January 2026.