Drug intelligence / Profile preview

ramelteon

Development stage
Approved
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

Ramelteon is a small molecule hypnotic medication indicated for the treatment of insomnia, specifically for patients who have difficulty with sleep onset. It acts as a selective agonist at melatonin MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN) of the hypothalamus, which are involved in regulating circadian rhythms and promoting sleep. Ramelteon has high affinity for these receptors, with greater selectivity over non-human MT3 receptors, and does not bind appreciably to GABAergic or other CNS receptor systems commonly associated with sedation. Its unique mechanism distinguishes it from traditional hypnotics such as benzodiazepines and Z-drugs. The drug was developed to mimic endogenous melatonin’s effects on sleep-wake cycles without significant risk of dependence or abuse[5][7][8].

Brand names
Rozerem
Other names
(S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide
02

Targets

MTNR1B (Melatonin Receptor 2)NQO2 (Ribosyldihydronicotinamide dehydrogenase [quinone])MTNR1A (MT1)

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