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Tasimelteon
Systematic (IUPAC) name
N-([(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl)propanamide
Identifiers
CAS number 609799-22-6
ATC code none
PubChem 10220503
Chemical data
Formula C 15H19NO2  
Mol. mass 245.3 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes Oral

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]

References

  1. ^ 'Time-bending drug' for jet lag. BBC News. 2 December 2008
  2. ^ Vachharajani NN, Yeleswaram K, Boulton DW. Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist. Journal of Pharmaceutical Sciences. 2003 Apr;92(4):760-72. PMID 12661062
  3. ^ Rajaratnam SMW, Polymeropoulos MH, Fisher DM, Roth T, Scott C, Birznieks G, Klerman EB. Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials. The Lancet Early Online Publication, 2 December 2008. doi:10.1016/S0140-6736(08)61812-7
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