Drug intelligence / Profile preview

tasimelteon

Development stage
Approved
Lead developer
Vanda Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Tasimelteon is a selective melatonin receptor agonist indicated for the treatment of non‑24‑hour sleep-wake disorder (Non‑24), primarily in totally blind adults, and for nighttime sleep disturbances in patients with Smith-Magenis Syndrome (SMS). It acts by binding to melatonin MT1 and MT2 receptors in the suprachiasmatic nucleus of the brain, helping to regulate circadian rhythms. Tasimelteon has greater affinity for the MT2 receptor than MT1. The drug is available as oral capsules and oral suspension; these formulations are not interchangeable. It was developed by Vanda Pharmaceuticals and first approved by the FDA in 2014[1][3][5][9].

Brand names
HetliozHetlioz LQ
Other names
tasimelteonumN-{[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl}propanamideTasimeltéonTasimelteón
02

Targets

MTNR1B (Melatonin Receptor 2)MTNR1A (MT1)

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