Journal article

Lemborexant Dual orexin receptor antagonist Treatment of insomnia

D Hoyer, LH Jacobson

DRUGS OF THE FUTURE | PROUS SCIENCE, SAU-THOMSON REUTERS | Published : 2018

Abstract

Eisai's lemborexant, or E-2006, is a dual orexin OX1/OX2 receptor antagonist (DORA)in codevelopment withPurdue Pharma. Functionally, lemborexant is about 10-fold selective for OX2 over OX1, whereas it is almost nonselective in recombinant human, rat and mouse receptor binding assays. Lemborexant binds and dissociates rapidly from orexin receptors in contrast to other DORAs, which are typically slow to dissociate. It is relatively stable, shows good bioavailability and brain penetration. In mice, lemborexant enhanced sleep for 4-5 h with effects on both non-REM and REM sleep. Lemborexant is currently in phase II/III clinical studies for the treatment of insomnia. A phase II proof-of-concept s..

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