Daridorexant

Daridorexant
Clinical data
Trade namesQuviviq
Other namesNemorexant; ACT-541468, Daridorexant hydrochloride (USAN US)
License data
Routes of
administration		By mouth[1]
Drug classDual orexin receptor antagonist; Hypnotic; Sedative
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability62%[1]
Protein binding99.7%[1]
MetabolismExtensive (mainly CYP3A4 (89%))[1]
Onset of actionTmax: 1–2 hours (delayed by 1.3 hours with food)[1]
Elimination half-life8 hours (6–10 hours)[1][5]
Duration of action~8 hours (50 mg)[5]
ExcretionFeces: ~57%[1]
Urine: ~28%[1]
Identifiers
  • [(2S)-2-(5-Chloro-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.353.123 Edit this at Wikidata
Chemical and physical data
FormulaC23H23ClN6O2
Molar mass450.93 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC2=C1N=C(N2)[C@@]3(CCCN3C(=O)C4=C(C=CC(=C4)OC)N5N=CC=N5)C)Cl
  • 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.[1][4][6][7][8] Daridorexant is taken by mouth.[1][4][7]

Side effects of daridorexant include headache, somnolence, and fatigue.[1][7] The medication is a dual orexin receptor antagonist (DORA).[9][7][10][8] It acts as a selective dual antagonist of the orexin receptors OX1 and OX2.[9][10][8] Daridorexant has a relatively short elimination half-life of 8 hours and a time to peak of about 1 to 2 hours.[1][7][5] It is not a benzodiazepine or Z-drug and does not interact with GABA receptors, instead having a distinct mechanism of action.[8][7]

Daridorexant was approved for medical use in the United States in January 2022[1][11] and became available in May 2022.[12] It was approved in the European Union in April 2022, and is the first orexin receptor antagonist to become available in European Union.[13] The medication is a schedule IV controlled substance in the United States and may have a modest potential for misuse.[1][14][15] Besides daridorexant, other orexin receptor antagonists, like suvorexant and lemborexant, have also been introduced.[16][17]

  1. ^ a b c d e f g h i j k l m n o "Quviviq- daridorexant tablet, film coated". DailyMed. 23 March 2022. Archived from the original on 19 September 2022. Retrieved 18 September 2022.
  2. ^ "Summary Basis of Decision for Quviviq". Health Canada. 4 August 2023. Retrieved 4 October 2023.
  3. ^ "Details for: Quviviq". Health Canada. 8 September 2023. Retrieved 4 October 2023.
  4. ^ a b c Cite error: The named reference Quviviq EPAR was invoked but never defined (see the help page).
  5. ^ a b c Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J (November 2020). "Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders". Expert Opinion on Drug Metabolism & Toxicology. 16 (11): 1063–1078. doi:10.1080/17425255.2020.1817380. PMID 32901578. S2CID 221572078.
  6. ^ "Quviviq Product Information" (PDF). European Medicines Agency. 2022. Archived (PDF) from the original on 6 May 2022. Retrieved 5 May 2022.
  7. ^ a b c d e f Park J, Render PharmD KP, Cates PharmD DW (January 2023). "Daridorexant: Comprehensive Review of A New Oral Agent for the Treatment of Insomnia". The Annals of Pharmacotherapy. 57 (9): 1076–1087. doi:10.1177/10600280221143794. PMID 36602018. S2CID 255473890.
  8. ^ a b c d Roch C, Bergamini G, Steiner MA, Clozel M (October 2021). "Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia". Psychopharmacology. 238 (10): 2693–2708. doi:10.1007/s00213-021-05954-0. PMC 8455402. PMID 34415378.
  9. ^ a b "Daridorexant - Idorsia Pharmaceuticals - AdisInsight". Archived from the original on 19 June 2018. Retrieved 19 June 2018.
  10. ^ a b Equihua-Benítez AC, Guzmán-Vásquez K, Drucker-Colín R (July 2017). "Understanding sleep-wake mechanisms and drug discovery". Expert Opinion on Drug Discovery. 12 (7): 643–657. doi:10.1080/17460441.2017.1329818. PMID 28511597. S2CID 3513546.
  11. ^ "Drug Approval Package: Quviviq". U.S. Food and Drug Administration (FDA). 14 February 2022. Archived from the original on 4 March 2022. Retrieved 4 March 2022.
  12. ^ "Idorsia's new treatment QUVIVIQ (Daridorexant) is now available in the US for adults living with insomnia" (Press release). 2 May 2022. Archived from the original on 5 May 2022. Retrieved 5 May 2022.
  13. ^ "Europe's first dual orexin receptor antagonist – Quviviq (Daridorexant) – granted approval to improve both nighttime symptoms and daytime functioning in adults with chronic insomnia disorder". 3 May 2022. Archived from the original on 5 May 2022. Retrieved 5 May 2022.
  14. ^ Cite error: The named reference Idorsia PR was invoked but never defined (see the help page).
  15. ^ "Schedules of Controlled Substances: Placement of Daridorexant in Schedule IV". Archived from the original on 13 April 2022. Retrieved 13 April 2022. Public Domain This article incorporates text from this source, which is in the public domain.
  16. ^ Cite error: The named reference pmid35043499 was invoked but never defined (see the help page).
  17. ^ Cite error: The named reference pmid35298826 was invoked but never defined (see the help page).