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Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
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Tasimelteon: a selective and unique receptor binding profile.

Christian Lavedan1, Mark Forsberg1, Anthony J Gentile2

  • 1Vanda Pharmaceuticals Inc., 2200 Pennsylvania Ave. N.W., Suite 300-E, Washington, D.C, 20037, USA.

Neuropharmacology
|December 24, 2014
PubMed
Summary

Tasimelteon (Hetlioz®) is a potent dual melatonin receptor agonist, showing higher affinity for the MT2 receptor involved in circadian rhythms. This drug is the first approved treatment for Non-24-Hour Sleep-Wake Disorder.

Keywords:
Circadian regulatorCircadian rhythmHetlioz(®)Melatonin receptorNon-24TasimelteonTasimelteon (PubChem CID:10220503)

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Area of Science:

  • Pharmacology
  • Chronobiology

Background:

  • Non-24-Hour Sleep-Wake Disorder (Non-24) is a circadian rhythm disorder.
  • Hetlioz® (tasimelteon) is the first FDA-approved treatment for Non-24.

Purpose of the Study:

  • To characterize the in vitro binding affinity of tasimelteon for human melatonin receptors MT1 and MT2.
  • To assess the binding profile of tasimelteon across a broad range of other receptors and enzymes.

Main Methods:

  • In vitro binding assays were performed to determine the affinity (Ki values) of tasimelteon for MT1 and MT2 receptors.
  • An extended screening panel evaluated tasimelteon's affinity for over 160 additional receptors and several enzymes.

Main Results:

  • Tasimelteon demonstrated potent dual agonism at both MT1 and MT2 receptors.
  • Tasimelteon exhibited 2.1-4.4 times greater affinity for the MT2 receptor (Ki = 0.0692-0.17 nM) compared to the MT1 receptor (Ki = 0.304-0.35 nM).
  • Tasimelteon showed no significant affinity for over 160 other pharmacologically relevant targets.

Conclusions:

  • Tasimelteon is a potent dual melatonin receptor agonist with preferential binding to MT2.
  • The drug's specific binding profile supports its efficacy in treating Non-24-Hour Sleep-Wake Disorder by targeting circadian rhythm regulation.