Drug intelligence / Profile preview

ramelteon + doxepin

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

Overview

Ramelteon + doxepin is a combination of two pharmaceutical drugs used primarily for the treatment of insomnia. Ramelteon is a selective melatonin receptor agonist that mimics the action of endogenous melatonin by binding to MT1 and MT2 receptors in the brain's suprachiasmatic nucleus, thereby regulating circadian rhythms and promoting sleep onset[1][4][6]. Doxepin is a tricyclic antidepressant with strong antihistaminic properties at low doses; it acts as an antagonist at histamine H1 receptors, which helps maintain sleep in patients with insomnia[8]. Both agents are not controlled substances and are generally considered non-habit-forming. Ramelteon was developed to target sleep initiation, while doxepin (at low doses) targets sleep maintenance.

02

Targets

5-HT2 (5-HT2 receptor family)HRH1 (Histamine H1 Receptor)MTNR1A (MT1)ADRA1A (α1A)mAChR (Muscarinic acetylcholine receptors)MTNR1B (Melatonin Receptor 2)

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