Drug intelligence / Profile preview

placebo + lemborexant

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

Overview

Placebo + lemborexant refers to the comparative treatment arms used in a clinical trial (specifically a randomized, double-blind, 6-way crossover study) to evaluate the abuse potential of lemborexant in recreational sedative users. Lemborexant, marketed under the brand name DAYVIGO, is a small molecule dual orexin receptor antagonist (DORA) developed by Eisai for the treatment of insomnia. It works by competitively binding to and inhibiting both orexin receptor subtypes, OX1R and OX2R, which are wake-promoting neuropeptide receptors involved in the regulation of the sleep-wake cycle. Unlike traditional sedative-hypnotics such as benzodiazepines or Z-drugs, lemborexant does not interact with GABA receptors. It was approved by the U.S. FDA in 2019 and is classified as a Schedule IV controlled substance due to its potential for abuse, which was the focus of the study involving the placebo comparator.

02

Targets

HCRTR1 (Orexin/hypocretin receptor type 1)HCRTR2 (Orexin/hypocretin receptor type 2)

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