Agomelatine, a melatonin agonist with antidepressant properties

Expert Opin Investig Drugs. 2009 Oct;18(10):1533-40. doi: 10.1517/13543780903292634.

Abstract

Agomelatine (beta-methyl-6-chloromelatonin), which is structurally homologous to melatonin, is a potent agonist of melatonin MT1 and MT2 receptors as well as an antagonist of serotonin 5-HT(2C) receptors. Agomelatine appears to improve sleep without causing daytime sedation. It has not been found to be associated with sexual side effects and discontinuation symptoms. Three placebo-controlled trials, one of them a dose finding study and two of them pivotal trials, suggest that agomelatine is an antidepressant at doses of 25 - 50 mg/day. Agomelatine appears to be well tolerated, without sexual or cardiac adverse effects, weight gain or discontinuation syndromes. Animal studies suggest a possible neuroprotective action of agomelatine, although there are more data in favor of an anxiolytic effect. Substantially more research is needed to establish its role in the treatment of mood and circadian rhythm disorders.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acetamides / adverse effects
  • Acetamides / pharmacology
  • Acetamides / therapeutic use*
  • Animals
  • Antidepressive Agents / adverse effects
  • Antidepressive Agents / pharmacology
  • Antidepressive Agents / therapeutic use*
  • Clinical Trials as Topic
  • Depressive Disorder, Major / drug therapy
  • Depressive Disorder, Major / physiopathology*
  • Humans
  • Receptor, Melatonin, MT1 / agonists
  • Receptor, Melatonin, MT2 / agonists
  • Serotonin 5-HT2 Receptor Antagonists
  • Sleep / drug effects

Substances

  • Acetamides
  • Antidepressive Agents
  • Receptor, Melatonin, MT1
  • Receptor, Melatonin, MT2
  • Serotonin 5-HT2 Receptor Antagonists
  • agomelatine