Tasimelteon, a melatonin agonist for the treatment of insomnia and circadian rhythm sleep disorders

Curr Opin Investig Drugs. 2009 Jul;10(7):691-701.


Tasimelteon, developed by Vanda Pharmaceuticals Inc under license from Bristol-Myers Squibb Co, is a melatonin receptor agonist. Because of the high density of melatonin receptors in the circadian pacemaker, the suprachiasmatic nucleus, melatonergic actions can phase-shift circadian rhythms and promote sleep. Tasimelteon was effective in reducing sleep onset latency (in phase II and III clinical trials) and in resetting the circadian melatonin rhythm (in phase II trials), which indicated its potential suitability as treatment for jet lag, shift work and circadian rhythm sleep disorders. Statistically significant improvements in sleep maintenance have also been observed with the drug. Tasimelteon has been claimed to be useful in the treatment of depression, and preclinical evidence in this respect is to be confirmed in a phase II clinical trial, which was ready to be initiated at the time of publication. It is plausible that the drug may be effective in the treatment of depressive disorders, at least those that are related to circadian dysfunction, and that it may attenuate sleep problems in depressed patients of different subtypes. A general suitability in mitigating other symptoms of major depressive disorder cannot be deduced from the actions of tasimelteon via the melatonin receptors MT1 and MT2. The drug is well tolerated, does not induce impairment of next-day functioning or dependence, and seems to be safe in short-term treatment; however, toxicological data would be required for assessing its long-term safety.

MeSH terms

  • Animals
  • Benzofurans / adverse effects
  • Benzofurans / chemistry
  • Benzofurans / pharmacokinetics
  • Benzofurans / therapeutic use*
  • Clinical Trials as Topic
  • Cyclopropanes / adverse effects
  • Cyclopropanes / chemistry
  • Cyclopropanes / pharmacokinetics
  • Cyclopropanes / therapeutic use*
  • Drugs, Investigational / therapeutic use
  • Humans
  • Melatonin / therapeutic use*
  • Molecular Structure
  • Patents as Topic
  • Receptors, Melatonin / agonists*
  • Sleep Disorders, Circadian Rhythm / drug therapy*
  • Sleep Initiation and Maintenance Disorders / drug therapy*
  • Structure-Activity Relationship


  • Benzofurans
  • Cyclopropanes
  • Drugs, Investigational
  • Receptors, Melatonin
  • Melatonin
  • tasimelteon