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

Abstract

Non-24-h sleep-wake rhythm disorder (non-24) is observed in approximately half of totally blind individuals, a condition caused by their circadian pacemaker in the suprachiasmatic nucleus not being entrained to 24 h due to a lack of light perceptions. These subjects have a progressively delayed circadian cycle each day, non-24 periodically inducing nighttime insomnia and daytime sleepiness. Tasimelteon is a dual melatonin receptor agonist with high affinity for the melatonin 2 receptor, and it entrains endogenous melatonin rhythms and sleep-wake cycles in individuals with non-24. Areas covered: Herein, the authors review the treatment of non-24 with tasimelteon. The authors further compare tasimelteon with other melatonin receptor agonists. Expert opinion: The treatment strategies for non-24 aim to resynchronize the free-running rhythm with the 24 h light-dark cycle. Tasimelteon entrains circadian rhythms and improves the sleep-wake functions of individuals with non-24. Furthermore, the RESET study demonstrated that 20% of patients that discontinued tasimelteon maintained circadian entrainment whereas 90% of those who continued it maintained circadian entrainment. Long-term administration of tasimelteon is safe and well tolerated, and it is the only pharmacological therapy approved by the US Food and Drug Administration and the European Medicines Agency for non-24.

Keywords: Circadian rhythm; melatonin; melatonin receptor agonist; non-24-h sleep-wake rhythm disorder tasimelteon.