Daridorexant

Daridorexant
Clinical data
Trade names	Quviviq
Other names	Nemorexant; ACT-541468, Daridorexant hydrochloride (USAN US)
License data	US DailyMed: Daridorexant;
Routes of; administration	By mouth
Drug class	Dual orexin receptor antagonist; Hypnotic; Sedative
ATC code	N05CJ03 (WHO) ;
Legal status
Legal status	CA: ℞-only; US: Schedule IV; EU: Rx-only;
Pharmacokinetic data
Bioavailability	62%
Protein binding	99.7%
Metabolism	Extensive (mainly CYP3A4 (89%))
Onset of action	Tmax: 1–2 hours (delayed by 1.3 hours with food)
Elimination half-life	8 hours (6–10 hours)
Duration of action	~8 hours (50 mg)
Excretion	Feces: ~57%; Urine: ~28%
Identifiers
	IUPAC name [(2S)-2-(5-Chloro-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone;
CAS Number	1505484-82-1; as HCl: 1792993-84-0;
PubChem CID	91801202; as HCl: 91809208;
IUPHAR/BPS	11648;
DrugBank	DB15031;
ChemSpider	64854514;
UNII	LMQ24G57E9; as HCl: 9X9581N56R;
KEGG	D11886; as HCl: D11887;
ChEMBL	ChEMBL4297590; as HCl: ChEMBL4650216;
PDB ligand	NS2 (PDBe, RCSB PDB);
ECHA InfoCard	100.353.123
Chemical and physical data
Formula	C23H23ClN6O2
Molar mass	450.93 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C=CC2=C1N=C(N2)[C@@]3(CCCN3C(=O)C4=C(C=CC(=C4)OC)N5N=CC=N5)C)Cl;
	InChI InChI=1S/C23H23ClN6O2/c1-14-17(24)6-7-18-20(14)28-22(27-18)23(2)9-4-12-29(23)21(31)16-13-15(32-3)5-8-19(16)30-25-10-11-26-30/h5-8,10-11,13H,4,9,12H2,1-3H3,(H,27,28)/t23-/m0/s1; Key:NBGABHGMJVIVBW-QHCPKHFHSA-N;

Daridorexant, sold under the brand name Quviviq, is an orexin antagonist medication which is used for the treatment of insomnia. Daridorexant is taken by mouth.

Side effects of daridorexant include headache, somnolence, and fatigue. The medication is a dual orexin receptor antagonist (DORA). It acts as a selective dual antagonist of the orexin receptors OX₁ and OX₂. Daridorexant has a relatively short elimination half-life of 8 hours and a time to peak of about 1 to 2 hours. It is not a benzodiazepine or Z-drug and does not interact with GABA receptors, instead having a distinct mechanism of action.

Daridorexant was approved for medical use in the United States in January 2022 and became available in May 2022. It was approved in the European Union in April 2022, and is the first orexin receptor antagonist to become available in European Union. The medication is a schedule IV controlled substance in the United States and may have a modest potential for misuse. Besides daridorexant, other orexin receptor antagonists, like suvorexant and lemborexant, have also been introduced.

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