Filorexant

Filorexant
Systematic (IUPAC) name
[(2R,5R)-5-{[(5-Fluoro-2-pyridinyl)oxy]methyl}-2-methyl-1-piperidinyl][5-methyl-2-(2-pyrimidinyl)phenyl]methanone
Identifiers
CAS Number 1088991-73-4
ATC code None
PubChem CID 25128145
ChemSpider 28528372
Chemical data
Formula C24H25FN4O2
Molar mass 420.479 g/mol

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.
  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.
  3. Peroutka SJ (January 2014). "Clinical trials update. 2013: year in review". Headache 54 (1): 189–94. doi:10.1111/head.12267. PMID 24400767.
  4. Cooper CK (March 2014). "Orexin Receptor Antagonists: Novel Hypnotic Agents". Ment. Health. Clin. 4 (2): 64. ISSN 2168-9709.
  5. "Randomized controlled trial of the orexin receptor antagonist filorexant for migraine prophylaxis.". Cephalalgia 35: 379–88. Aug 8, 2014. doi:10.1177/0333102414544979. PMID 25106663.
  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.
This article is issued from Wikipedia - version of the Thursday, December 17, 2015. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.