Filorexant

Filorexant
Clinical data
Routes of
administration		By mouth
Drug classOrexin antagonist
ATC code
  • None
Identifiers
IUPAC name
  • [(2R,5R)-5-{[(5-Fluoro-2-pyridinyl)oxy]methyl}-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]methanone
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.203.042
Edit this at Wikidata
Chemical and physical data
FormulaC24H25FN4O2
Molar mass420.488 g·mol−1
3D model (JSmol)
SMILES
  • C[C@@H]1CC[C@H](CN1C(=O)C2=C(C=CC(=C2)C)C3=NC=CC=N3)COC4=NC=C(C=C4)F
InChI
  • InChI=1S/C24H25FN4O2/c1-16-4-8-20(23-26-10-3-11-27-23)21(12-16)24(30)29-14-18(6-5-17(29)2)15-31-22-9-7-19(25)13-28-22/h3-4,7-13,17-18H,5-6,14-15H2,1-2H3/t17-,18-/m1/s1
  • Key:NPFDWHQSDBWQLH-QZTJIDSGSA-N

Filorexant (INN, USAN) (code name MK-6096) is an orexin antagonist which is or was under development by Merck for the treatment of insomnia.[1] It is a dual antagonist of the OX1 and OX2 receptors.[2][3] As of March 2014, filorexant has completed phase II clinical trials.[4] It was also investigated as a migraine prophylaxis, but was not found effective,[5] and in major depressive disorder and painful diabetic neuropathy.[6] As of May 2015, filorexant is no longer listed on Merck's online development pipeline.[7]

See also

References

  1. ↑ Hoyer D, Jacobson LH (December 2013). "Orexin in sleep, addiction and more: is the perfect insomnia drug at hand?". Neuropeptides. 47 (6): 477–88. doi:10.1016/j.npep.2013.10.009. PMID 24215799. S2CID 6402764.
  2. ↑ Winrow CJ, Gotter AL, Cox CD, et al. (February 2012). "Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia". Neuropharmacology. 62 (2): 978–87. doi:10.1016/j.neuropharm.2011.10.003. PMID 22019562. S2CID 35304627.
  3. ↑ Peroutka SJ (January 2014). "Clinical trials update. 2013: year in review". Headache. 54 (1): 189–94. doi:10.1111/head.12267. PMID 24400767. S2CID 28141555.
  4. ↑ Cooper CK (March 2014). "Orexin Receptor Antagonists: Novel Hypnotic Agents". Ment. Health Clin. 4 (2): 64. doi:10.9740/mhc.n190094. ISSN 2168-9709.
  5. ↑ Chabi, A.; Zhang, Y.; Jackson, S.; Cady, R.; Lines, C.; Herring, W. J.; Connor, K. M.; Michelson, D. (Aug 8, 2014). "Randomized controlled trial of the orexin receptor antagonist filorexant for migraine prophylaxis". Cephalalgia. 35 (5): 379–88. doi:10.1177/0333102414544979. PMID 25106663. S2CID 20872932.
  6. ↑ Michel Alexander Steiner; Christopher J Winrow (11 November 2014). Insomnia and beyond - Exploring the therapeutic potential of orexin receptor antagonists. Frontiers E-books. pp. 3–. ISBN 978-2-88919-330-1.
  7. ↑ "Merck Pipeline". Merck. 2015. Retrieved 2015-05-14.


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