Daridorexant

Daridorexant (developmental code name ACT-541468), formerly known as nemorexant, is a dual orexin receptor antagonist (DORA) which was originated by Actelion Pharmaceuticals and is under development by Idorsia Pharmaceuticals for the treatment of insomnia.[2][3] It acts as a selective dual antagonist of the orexin receptors OX1 and OX2.[2][3] The medication has a relatively short elimination half-life of 6 to 10 hours.[1] As of April 2020, daridorexant has passed its first phase III clinical trial for the treatment of insomnia.[2]

Daridorexant
Clinical data
Other namesNemorexant; ACT-541468
Routes of
administration		By mouth
Drug classOrexin antagonist
Pharmacokinetic data
Elimination half-life6–10 hours[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
  • 1505484-82-1
PubChem CID
ChemSpider
UNII
KEGG
PDB ligand
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

See also

References
  1. 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 Opin Drug Metab Toxicol. 16 (11): 1063–1078. doi:10.1080/17425255.2020.1817380. PMID 32901578.
  2. "Daridorexant - Idorsia Pharmaceuticals - AdisInsight".
  3. Equihua-Benítez AC, Guzmán-Vásquez K, Drucker-Colín R (July 2017). "Understanding sleep-wake mechanisms and drug discovery". Expert Opin Drug Discov. 12 (7): 643–657. doi:10.1080/17460441.2017.1329818. PMID 28511597.



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