Tasimelteon

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Tasimelteon
Systematic (IUPAC) name
N-([(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl)propanamide
Clinical data
Pregnancy cat.  ?
Legal status  ?
Routes Oral
Identifiers
CAS number 609799-22-6
ATC code None
PubChem CID 10220503
UNII SHS4PU80D9 YesY
Chemical data
Formula C15H19NO2 
Mol. mass 245.3 g/mol
 YesY (what is this?)  (verify)

Tasimelteon (BMS-214,778) is a drug which is under development for the treatment of insomnia and other sleep disorders.[1] It is a selective agonist for the melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, similar to older drugs such as ramelteon.[2] It has been through Phase III trials successfully and was shown to improve both onset and maintenance of sleep, with few side effects.[3]

A year-long (2011-2012) study at Harvard is testing the use of tasimelteon in blind subjects with non-24-hour sleep-wake disorder.[4]

[edit] See also

Discovery and development of melatonin receptor agonists

[edit] References

  1. ^ 'Time-bending drug' for jet lag. BBC News. 2 December 2008
  2. ^ Vachharajani, Nimish N., Yeleswaram, Krishnaswamy, Boulton, David W. (April 2003). "Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist". Journal of Pharmaceutical Sciences 92 (4): 760–72. doi:10.1002/jps.10348. PMID 12661062. 
  3. ^ Shantha MW Rajaratnam, Mihael H Polymeropoulos, Dennis M Fisher, Thomas Roth, Christin Scott, Gunther Birznieks, Elizabeth B Klerman (2009-02-07). "Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials". The Lancet 373 (9662): 482–491. doi:10.1016/S0140-6736(08)61812-7. PMID 19054552. Retrieved 2010-02-23. 
  4. ^ Audio interview with Joseph Hull of Harvard, spring 2011