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MK4305 structure.png
Systematic (IUPAC) name
Clinical data
Legal status
  • Rx Only
CAS number 1030377-33-3 N
ATC code None
PubChem CID 24965990
ChemSpider 24662178 N
Chemical data
Formula C23H23ClN6O2 
Mol. mass 450.920 g/mol (free base)
 N (what is this?)  (verify)

Suvorexant (Belsomra) is a selective dual orexin receptor antagonist marketed by Merck & Co. for the treatment of insomnia.[1][2][3] The drug (originally known as MK-4305) completed three phase III trials[4] and was approved for sale by the U.S. Food & Drug Administration on August 13, 2014.[5] In the United States, the DEA has placed suvorexant on the list of schedule IV controlled substances, with an effective date of September 29, 2014.[6] Merck has said that it expects the drug to be available in late 2014 or early 2015.

Medical uses[edit]

Suvorexant is used for the treatment of insomnia, characterized by difficulties with sleep onset and/or sleep maintenance.[7]

Mechanism of action[edit]

Suvorexant exerts its therapeutic effect in insomnia through antagonism of orexin receptors. The orexin neuropeptide signaling system is a central promoter of wakefulness. Blocking the binding of wake-promoting neuropeptides orexin A and orexin B to receptors orexin receptor type 1 and orexin receptor type 2 is thought to suppress wake drive.[7]


  1. ^ Cox, C. D.; Breslin, M. J.; Whitman, D. B.; Schreier, J. D.; McGaughey, G. B.; Bogusky, M. J.; Roecker, A. J.; Mercer, S. P.; Bednar, R. A.; Lemaire, W.; Bruno, J. G.; Reiss, D. R.; Harrell, C. M.; Murphy, K. L.; Garson, S. L.; Doran, S. M.; Prueksaritanont, T.; Anderson, W. B.; Tang, C.; Roller, S.; Cabalu, T. D.; Cui, D.; Hartman, G. D.; Young, S. D.; Koblan, K. S.; Winrow, C. J.; Renger, J. J.; Coleman, P. J. (2010). "Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia". Journal of Medicinal Chemistry 53 (14): 5320–5332. doi:10.1021/jm100541c. PMID 20565075.  edit
  2. ^ Baxter, C. A.; Cleator, E.; Brands, K. M. J.; Edwards, J. S.; Reamer, R. A.; Sheen, F. J.; Stewart, G. W.; Strotman, N. A.; Wallace, D. J. (2011). "The First Large-Scale Synthesis of MK-4305: A Dual Orexin Receptor Antagonist for the Treatment of Sleep Disorder". Organic Process Research & Development 15 (2): 367–375. doi:10.1021/op1002853.  edit
  3. ^ Winrow, C. J.; Gotter, A. L.; Cox, C. D.; Doran, S. M.; Tannenbaum, P. L.; Breslin, M. J.; Garson, S. L.; Fox, S. V.; Harrell, C. M.; Stevens, J.; Reiss, D. R.; Cui, D.; Coleman, P. J.; Renger, J. J. (2011). "Promotion of Sleep by Suvorexant—A Novel Dual Orexin Receptor Antagonist". Journal of Neurogenetics 25 (1–2): 52–61. doi:10.3109/01677063.2011.566953. PMID 21473737.  edit
  4. ^ Three completed trials:
  5. ^
  6. ^
  7. ^ a b ""Highlights of prescribing information"".