Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials

  title={Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials},
  author={Shantha M. W. Rajaratnam and M. H. Polymeropoulos and Dennis M. Fisher and Thomas Roth and Christine Scott and Gunther Birznieks and Elizabeth B. Klerman},
  journal={The Lancet},

Efficacy of melatonin with behavioural sleep-wake scheduling for delayed sleep-wake phase disorder: A double-blind, randomised clinical trial

Melatonin treatment 1 h prior to DBT combined with behavioural sleep-wake scheduling was efficacious for improving objective and subjective measures of sleep disturbances and sleep-related impairments in DSWPD patients with delayed circadian phase relative to D BT.

Tasimelteon: a melatonin receptor agonist for non-24-hour sleep-wake disorder.

Tasimelteon improves sleep initiation and maintenance in patients with Non-24 who have a shift in endogenous circadian rhythms, however, the cost of this agent limits its use.

Efficacy of Tasimelteon (HETLIOZ®) in the Treatment of Jet Lag Disorder Evaluated in an 8-h Phase Advance Model; a Multicenter, Randomized, Double-Blind, Placebo-Controlled Trial

A single dose of tasimelteon improves the primary symptoms of Jet Lag Disorder, including nighttime insomnia and next day functioning among participants in a laboratory model of JLD simulating eastward trans-meridian travel by inducing an 8-h phase advance of the sleep-wake cycle.

Tasimelteon: A Review in Non-24-Hour Sleep-Wake Disorder in Totally Blind Individuals

People with Non-24 who received oral tasimelteon 20 mg once nightly were significantly more likely than those receiving placebo to entrain the circadian pacemaker and maintain entrainment in the RESET trial.

Tasimelteon (HETLIOZ®) effective in the treatment of Jet Lag Disorder in an 8-hour phase advance; a multicenter, randomized, double-blind, placebo-controlled trial

A single dose of tasimelteon improves symptoms, including sleep and next day functioning in participants, following an 8-h phase advance of the sleep-wake cycle in a laboratory model of JLD simulating eastward trans-meridian travel.

New approaches in the management of insomnia: weighing the advantages of prolonged-release melatonin and synthetic melatoninergic agonists

  • R. Hardeland
  • Psychology, Biology
    Neuropsychiatric disease and treatment
  • 2009
Despite otherwise good tolerability, the use of melatoninergic drugs in children, adolescents, and during pregnancy has been a matter of concern, and should be avoided in autoimmune diseases and Parkinsonism.

Tasimelteon for treating non-24-h sleep-wake rhythm disorder

Tasimelteon entrains circadian rhythms and improves the sleep-wake functions of individuals with non-24, and it is the only pharmacological therapy approved by the US Food and Drug Administration and the European Medicines Agency for non- 24.

Melatonergic agents influence the sleep-wake and circadian rhythms in healthy and psychiatric participants: a systematic review and meta-analysis of randomized controlled trials

Given the unmet clinical need for evidence-based treatments to correct circadian rhythms in psychiatric disorders, efficacy of melatonergic agents seen in healthy participants, and similarity of findings among psychiatric patients, large scale, well-designed randomized controlled trials are needed to test efficacy on circadian parameters in psychiatric Disorders.

Safety profile of tasimelteon, a melatonin MT1 and MT2 receptor agonist: pooled safety analyses from six clinical studies

Long-term tasimelteon administration was safe and well-tolerated, supported by placebo-controlled data in both Non-24 and insomnia patients.



Sleep-facilitating effect of exogenous melatonin in healthy young men and women is circadian-phase dependent.

The hypothesis that both exogenous and endogenousmelatonin attenuate the wake-promoting drive from the circadian system is supported, allowing for improved consolidation of sleep that occurs out of phase with endogenous melatonin secretion during the circadian night.

Zolpidem in the treatment of transient insomnia: a double-blind, randomized comparison with placebo.

It is demonstrated that zolpidem at 7.5 mg and 10 mg is effective in the treatment of transient insomnia, which may be induced by stress, sleep in unfamiliar surroundings, jet lag and other factors.

Ramelteon (TAK-375), a selective MT1/MT2-receptor agonist, reduces latency to persistent sleep in a model of transient insomnia related to a novel sleep environment.

Ramelteon significantly improved latency to persistent sleep and total sleep time in this model of transient insomnia in healthy adults and both doses were well tolerated.

Comparative efficacy of zolpidem and temazepam in transient insomnia

Zolpidem 10 mg provided greater subjective hypnotic efficacy than temazepam 15‬mg in this model of transient insomnia, with reduced polysomnographic awakenings and WASO, and both agents improved sleep efficiency and most subjective sleep measures relative to placebo.

Evaluation of the efficacy and safety of ramelteon in subjects with chronic insomnia.

Ramelteon reduced LPS over 5 weeks of treatment in subjects with chronic insomnia, with no clinically meaningful sleep architecture alterations, next-morning residual pharmacologic effects, and no evidence of rebound insomnia or withdrawal.

Sleep-promoting and hypothermic effects of daytime melatonin administration in humans.

It is suggested that melatonin may be an effective method of promoting sleep for individuals attempting to sleep during their subjective day, such as shiftworkers and individuals rapidly traveling across multiple time zones.

Effects of low oral doses of melatonin, given 2-4 hours before habitual bedtime, on sleep in normal young humans.

Observations provide additional evidence that nocturnal melatonin secretion has a sleep-promoting function and indicate that an increase in serum melatonin concentrations, within the normal physiologic range, does not significantly alter sleep architecture in subjects with normal sleep who receive the treatment several hours prior to their habitual bedtime.

Early evening melatonin and S-20098 advance circadian phase and nocturnal regulation of core body temperature.

The data suggest that, in addition to immediate thermoregulatory changes, a phase advance of the circadian system had occurred and that the phase advance could still be measured on the posttreatment day.

Effect of inducing nocturnal serum melatonin concentrations in daytime on sleep, mood, body temperature, and performance.

The data indicate that orally administered melatonin can be a highly potent hypnotic agent and suggest that the physiological increase in serum melatonin levels, which occurs around 2100 h daily, may constitute a signal initiating normal sleep onset.

The efficacy and safety of exogenous melatonin for primary sleep disorders a meta-analysis

There is evidence to suggest that melatonin is not effective in treating most primary sleep disorders with short-term use (4 weeks or less); however, additional large-scale RCTs are needed before firm conclusions can be drawn.