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lemborexant

Development stage: Approved
Lead developer: Eisai
Modality: Small Molecules
Administration: Oral

Overview

Lemborexant is a small molecule dual orexin receptor antagonist indicated for the treatment of insomnia, specifically for patients who have difficulty with sleep onset and/or sleep maintenance. It works by competitively blocking the binding of wake-promoting neuropeptides orexin A and orexin B to their receptors (Orexin receptor type 1 (OX1R) and Orexin receptor type 2 (OX2R)) in the brain, thereby suppressing wake drive and promoting sleep. Unlike traditional hypnotics that enhance GABAergic activity, lemborexant targets the underlying mechanism of inappropriate wakefulness. The drug was discovered and developed by Eisai[3][4][5][6][8].

Brand names: Dayvigo
Other names: LEM 5LEM5LEM-5Dayvigo 5 mgDayvigo5 mgDayvigo-5 mg

Targets

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

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