Lemborexant

Lemborexant
Clinical data
Trade names	Dayvigo
Other names	E-2006
License data	US DailyMed: Lemborexant;
Pregnancy; category	AU: B3;
Routes of; administration	By mouth
Drug class	Orexin receptor antagonist; Hypnotic; Sedative
ATC code	N05CJ02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; US: Schedule IV;
Pharmacokinetic data
Bioavailability	Good (≥87%)
Protein binding	94%
Metabolism	Liver (major: CYP3A4, minor: CYP3A5)
Metabolites	M10
Elimination half-life	17–19 hours or 55 hours
Excretion	Feces: 57.4%; Urine: 29.1%
Identifiers
	IUPAC name (1R,2S)-2-[(2,4-Dimethylpyrimidin-5-yl)oxymethyl]-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropane-1-carboxamide;
CAS Number	1369764-02-2;
PubChem CID	56944144;
IUPHAR/BPS	9302;
DrugBank	DB11951;
ChemSpider	34500836;
UNII	0K5743G68X;
KEGG	D11022;
ChEMBL	ChEMBL3545367;
Chemical and physical data
Formula	C22H20F2N4O2
Molar mass	410.425 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=NC(=NC=C1OC[C@]2(C[C@H]2C(=O)NC3=NC=C(C=C3)F)C4=CC(=CC=C4)F)C;
	InChI InChI=1S/C22H20F2N4O2/c1-13-19(11-25-14(2)27-13)30-12-22(15-4-3-5-16(23)8-15)9-18(22)21(29)28-20-7-6-17(24)10-26-20/h3-8,10-11,18H,9,12H2,1-2H3,(H,26,28,29)/t18-,22+/m0/s1; Key:MUGXRYIUWFITCP-PGRDOPGGSA-N;

Lemborexant, sold under the brand name Dayvigo, is an orexin antagonist medication which is used in the treatment of insomnia. It is indicated specifically for the treatment of insomnia characterized by difficulties with sleep onset and/or maintenance in adults. The medication is taken by mouth.

Side effects of lemborexant include somnolence, fatigue, headache, and abnormal dreams. The medication is a dual orexin receptor antagonist (DORA). It acts as a selective dual antagonist of the orexin receptors OX₁ and OX₂. Lemborexant has a long elimination half-life of 17 to 55 hours and a time to peak of about 1 to 3 hours. It is not a benzodiazepine or Z-drug and does not interact with GABA receptors, instead having a distinct mechanism of action.

Lemborexant was approved for medical use in the United States in December 2019. It is a schedule IV controlled substance in the United States and may have a low potential for misuse. Besides lemborexant, other orexin receptor antagonists including suvorexant and daridorexant have also been introduced.

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