PharmacotherapyAug 9, 2016

Comparison of Approved Melatonin-Like Medicines for Treating Sleep-Wake Cycle Disorders

Circadian Biology Weekly Brief ↗PubMed ↗DOI ↗OA ↗

Updated Mar 27, 2026

Abstract

(CRSWDs) affect millions and have a significant negative impact on quality of life.

Melatonin agonists may help shift and stabilize the circadian phase, presenting potential treatments for CRSWDs.
Currently, only tasimelteon is approved for treating non-24-hour sleep-wake disorder.
Agomelatine, prolonged-release melatonin, and ramelteon have been investigated as additional treatment options.
Distinct pharmacologic profiles of may clarify their clinical use in CRSWDs.
Further studies are needed to explore the therapeutic potential of these melatonin agonists for most CRSWDs.

Simplified

(CRSWDs) are characterized by persistent or recurrent patterns of sleep disturbance related primarily to alterations of the circadian rhythm system or the misalignment between the endogenous circadian rhythm and exogenous factors that affect the timing or duration of sleep. These disorders collectively represent a significant unmet medical need, with a total prevalence in the millions, a substantial negative impact on quality of life, and a lack of studied treatments for most of these disorders. Activation of the endogenous melatonin receptors appears to play an important role in setting the circadian clock in the suprachiasmatic nucleus of the hypothalamus. Therefore, melatonin agonists, which may be able to shift and/or stabilize the circadian phase, have been identified as potential therapeutic candidates for the treatment of CRSWDs. Currently, only one melatonin receptor agonist, tasimelteon, is approved for the treatment of a CRSWD: non-24-hour sleep-wake disorder (or non-24). However, three additional commercially available -agomelatine, prolonged-release melatonin, and ramelteon-have been investigated for potential use for treatment of CRSWDs. Data indicate that these melatonin receptor agonists have distinct pharmacologic profiles that may help clarify their clinical use in CRSWDs. We review the pharmacokinetic and pharmacodynamic properties of these melatonin agonists and summarize their efficacy profiles when used for the treatment of CRSWDs. Further studies are needed to determine the therapeutic potential of these melatonin agonists for most CRSWDs.

Key numbers

20 mg

Efficacy of Tasimelteon

Dosing for tasimelteon in clinical trials.

110

Study Participants for Jet Lag

Participants in the placebo-controlled study of ramelteon.

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Comparison of Approved Melatonin-Like Medicines for Treating Sleep-Wake Cycle Disorders

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