Lemborexant
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Lemborexant, sold under the brand name Dayvigo, is an orexin antagonist medication which is used in the treatment of insomnia.[3][8] It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults.[3][8] The medication is taken by mouth.[3][8]
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Trade names | Dayvigo |
Other names | E-2006 |
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Routes of administration | By mouth[3] |
Drug class | Orexin receptor antagonist; Hypnotic; Sedative |
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Bioavailability | Good (≥87%)[5][6] |
Protein binding | 94%[3] |
Metabolism | Liver (major: CYP3A4, minor: CYP3A5)[3] |
Metabolites | M10[3] |
Elimination half-life | 17–19 hours or 55 hours[3][7] |
Excretion | Feces: 57.4%[3] Urine: 29.1%[3] |
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Formula | C22H20F2N4O2 |
Molar mass | 410.425 g·mol−1 |
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Side effects of lemborexant include somnolence, fatigue, headache, and abnormal dreams.[3][8] The medication is a dual orexin receptor antagonist (DORA).[3][8] It acts as a selective dual antagonist of the orexin receptors OX1 and OX2.[3][8] Lemborexant has a long elimination half-life of 17 to 55 hours and a time to peak of about 1 to 3 hours.[3][8] It is not a benzodiazepine or Z-drug and does not interact with GABA receptors, instead having a distinct mechanism of action.[3][8]
Lemborexant was approved for medical use in the United States in December 2019.[9][10][11] It is a schedule IV controlled substance in the United States and may have a low potential for misuse.[3][8] Besides lemborexant, other orexin receptor antagonists including suvorexant and daridorexant have also been introduced.[12][13]