{"ATC Code":["N - Nervous system","N05 - Psycholeptics","N05C - Hypnotics and sedatives","N05CJ - Orexin receptor antagonists","N05CJ03 - Daridorexant","QN - Nervous system","QN05 - Psycholeptics","QN05C - Hypnotics and sedatives","QN05CJ - Orexin receptor antagonists","QN05CJ03 - Daridorexant"],"Absorption, Distribution and Excretion":"Daridorexant reaches peak plasma concentrations within one to two hours. Daridorexant has an absolute bioavailability of 62%. While a high-fat and high-calorie meal delayed the Tmax by 1.3 hours and decreased the Cmax by 16% in healthy subjects, the total exposure (AUC) was not affected.","Aliases":["Nemorexant","ACT-541468","Quviviq","Dea no. 2410","Methanone, ((2S)-2-(6-chloro-7-methyl-1H-benzimidazol-2-yl)-2-methyl-1-pyrrolidinyl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)-","daridorexantum","((2S)-2-(5-chloro-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl)-(5-methoxy-2-(triazol-2-yl)phenyl)methanone","Dtxcid901766549","((S)-(2-(5-chloro-4-methyl-1H-benzo(d)imidazol-2-yl)-2-methylpyrrolidin-1-yl) (5 methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone)","5-chloro-2-((2S)-1-(5-methoxy-2-(2H-1,2,3-triazol-2-yl)benzoyl)-2-methylpyrrolidin-2-yl)-4-methyl-1H-1,3-benzodiazole","methanone, ((2S)-2-(6-chloro-7-methyl-1H-benzimidazol-2-yl)-2-methyl-1-pyrrolidinyl)(5-methoxy-2-(2H-1,2,3-traizol-2-yl)phenyl)-","Mfcd31630772","Act 541468;act-541468","[2-(6-Chloro-7-methyl-2-benzimidazolyl)-2-methyl-1-pyrrolidinyl][5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone","[(2~{S})-2-(6-chloranyl-7-methyl-1~{H}-benzimidazol-2-yl)-2-methyl-pyrrolidin-1-yl]-[5-methoxy-2-(1,2,3-triazol-2-yl)phenyl]methanone","Nemorexant?","ACT541468","Daridorexant free base","Nemorexant;?Daridorexant","nemorexant","orb1473166","Chembl4297590","Schembl16766318","Schembl16778804","Schembl30028832","EX-A7813A","GTPL11648","BDBM334973","GLXC-15297","FKC48482","WHO 10679","US9732075, Example 5.36","Akos040742277","DB15031","[(2S)-2-(5-chloro-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl][5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone","DA-66016","SY251586","HY-109095","CS-0039396","(2S)-2-(5-chloro-4-methyl-1h-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone","(s)-(2-(5-chloro-4-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5 methoxy-2-(2h-1,2,3-triazol-2-yl)phenyl)methanone","(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone","2-(5-chloro-4-methyl-1H benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl](5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone","[(2S)-2-(5-chloro-4-methyl-1H-benzimidazol-2-yl)-2-methyl-pyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone","[(S)-2-(5-Chloro-4-methyl-1H-benzoimidazol-2-yl)-2-methyl-pyrrolidin-1-yl]-(5-methoxy-2-[1,2,3]triazol-2-yl-phenyl)-methanone","Daridorexant; (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone"],"Biological Half-Life":"The terminal half-life is approximately 8 hours.","CAS":"1505484-82-1","ChemicalClasses":["benzylamine"],"Chirality":"absolute","DTXSID":"701336356","Drug Classes":["Breast Feeding","Lactation","Milk, Human","Hypnotics and Sedatives","Orexin Receptor Antagonists","Sleep Aids, Pharmaceutical"],"Drug Indication":"In the US and Europe, daridorexant is indicated for the treatment of adult patients with insomnia characterized by difficulties with sleep onset and/or sleep maintenance. The European prescribing information states that insomnia should be characterized by symptoms that are present for at least three months and have a considerable impact on daytime functioning.","DurationOfAction":"~8 hours (50 mg)","EliminationHalfLife":"8 hours (6 – 10 hours)\u003ca href='#cite_note-6'\u003e\u003csup\u003e[6]\u003c/sup\u003e\u003c/a\u003e","Esters":[],"European Community (EC) Number":"879-120-8","FDA Pharmacological Classification":[{"Name":"FDA UNII","ReferenceNumber":20,"Value":{"StringWithMarkup":[{"String":"LMQ24G57E9"}]}},{"Name":"Active Moiety","ReferenceNumber":20,"Value":{"StringWithMarkup":[{"String":"DARIDOREXANT"}]}},{"Name":"Pharmacological Classes","ReferenceNumber":20,"Value":{"StringWithMarkup":[{"String":"Established Pharmacologic Class [EPC] - Orexin Receptor Antagonist"}]}},{"Name":"Pharmacological Classes","ReferenceNumber":20,"Value":{"StringWithMarkup":[{"String":"Mechanisms of Action [MoA] - Orexin Receptor Antagonists"}]}},{"Name":"FDA Pharmacology Summary","ReferenceNumber":20,"Value":{"StringWithMarkup":[{"Markup":[{"Extra":"CID-91801202","Length":12,"Start":0,"Type":"PubChem Internal Link","URL":"https://pubchem.ncbi.nlm.nih.gov/compound/Daridorexant"},{"Extra":"CID-91801202","Length":12,"Start":74,"Type":"PubChem Internal Link","URL":"https://pubchem.ncbi.nlm.nih.gov/compound/daridorexant"}],"String":"Daridorexant is an Orexin Receptor Antagonist. The mechanism of action of daridorexant is as an Orexin Receptor Antagonist."}]}},{"Name":"Non-Proprietary Name","ReferenceNumber":26,"Value":{"StringWithMarkup":[{"String":"DARIDOREXANT"}]}},{"Name":"Pharmacological Classes","ReferenceNumber":26,"Value":{"StringWithMarkup":[{"String":"Orexin Receptor Antagonists [MoA]; Orexin Receptor Antagonist [EPC]"}]}}],"Formating":[],"HeavyAtomCount":32,"Human Drugs":"Breast Feeding; Lactation; Milk, Human; Hypnotics and Sedatives; Orexin Receptor Antagonists; Sleep Aids, Pharmaceutical","IUPACName":"[(2S)-2-(5-chloro-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone","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","InChIKey":"NBGABHGMJVIVBW-QHCPKHFHSA-N","MeSH Headers":[{"Id":"M000655638","Link":"https://id.nlm.nih.gov/mesh/M000655638.html","Name":"daridorexant","Ref":41},{"Id":"M000655637","Link":"https://id.nlm.nih.gov/mesh/M000655637.html","Name":"ACT-541468","Ref":43},{"Id":"DescTree","Link":"https://www.nlm.nih.gov/mesh/meshhome.html","Name":"MeSH Tree","Ref":44},{"Id":"PubMed from MeSH","Link":"https://www.nlm.nih.gov/mesh/meshhome.html","Name":null,"Ref":61}],"Mechanism of Action":"The sleep and wake cycle is regulated by complex interactions between sleep-promoting systems, including inhibitory GABA activity, and wake-promoting systems, including orexins, acetylcholine and monoaminergic systems. Orexin, also called hypocretin, is a wake-promoting neuropeptide produced by a small group of neurons in the lateral hypothalamus. Orexin stabilizes wakefulness by activating orexin neurons with the highest activity during active wakefulness and minimal activity during sleep. Orexin neurons project to other wake-promoting neurons that also express orexin receptors: these include the histaminergic neurons of the tuberomammillary nucleus, noradrenergic neurons of the locus coeruleus, serotoninergic neurons of the dorsal raphe, dopaminergic neurons of the ventral tegmental area, and cholinergic neurons of the basal forebrain and the pedunculopontine and laterodorsal tegmental nuclei. These wake-promoting neurons are part of the ascending reticular activating system that operates under a feedback loop in the sleep and wake cycle.   There are two identified types of orexin (OXA and OXB) that bind to orexin type 1 and 2 receptors (OX1R and OX2R), which are G-protein coupled receptors. OXA binds more preferentially to OX1R, while OX2R shows a dual affinity for OXA and OXB. The defined role of each orexin receptor is still unclear; however, there is some evidence suggesting that OX2R regulates sleep and wake, while OX1R have some role in sleep maintenance. Daridorexant blocks the binding of wake-promoting neuropeptides OXA and OXB to OX1R and OX2R, thereby suppressing wake drive. Daridorexant selectively targets orexin neurons and inhibits downstream neuronal pathways that promote wakefulness; however, it does not affect neuronal pathways that cause side effects commonly seen in positive allosteric GABA-A receptor modulators.","Metabolism/Metabolites":"Daridorexant undergoes extensive metabolism primarily mediated by CYP3A4 (89%), mostly via oxidative transformations. Other CYP enzymes individually contribute to less than 3% of metabolic clearance of daridorexant.","MolecularFormula":"C\u003csub\u003e23\u003c/sub\u003eH\u003csub\u003e23\u003c/sub\u003eClN\u003csub\u003e6\u003c/sub\u003eO\u003csub\u003e2\u003c/sub\u003e","MolecularWeight":"450.9 g/mol","Opticalactivity":"UNSPECIFIED","Pharmacodynamics":"Daridorexant binds to and antagonizes the orexin receptors OX1R and OX2R (Ki = 0.47 and 0.93 nM, respectively) equipotentally. In clinical trials, daridorexant improved sleep onset and sleep maintenance, and patient-reported total sleep time. Patient-reported daytime sleepiness was also reportedly reduced. At a dose four times the maximum recommended dose, daridorexant does not prolong the QTc interval to any clinically relevant extent.  Daridorexant is currently being assessed for a controlled substance schedule in the US. In a human abuse potential study, daridorexant showed some abuse potential at doses higher than the recommended dose (100-150 mg), indicated by similar “drug liking” ratings to zolpidem (30 mg) and suvorexant in recreational sedative drug users. However, at clinically relevant concentrations, daridorexant does not bind to abuse-associated CNS targets. In animal studies and clinical trials evaluating physical dependence, chronic administration of daridorexant did not produce withdrawal signs or symptoms upon drug discontinuation, indicating that the drug does not produce physical dependence.","PubChemId":91801202,"PubChemTitle":"Daridorexant","Records":{"UNII":{"Impurities":[]}},"RefChem":"56310","RefCount":7,"RefCur":"","References":[{"Name":"Wikipedia","Urls":[{"Link":"https://en.wikipedia.org/wiki/Daridorexant","Name":"Daridorexant","Sub":false}]},{"Name":"Wikidata","Urls":[{"Link":"https://www.wikidata.org/wiki/Q55112806","Name":"Daridorexant","Sub":false}]},{"Name":"DrugBank","Urls":[{"Link":"https://go.drugbank.com/DB15031","Name":"Daridorexant","Sub":false}]},{"Name":"PubChem","Urls":[{"Link":"https://pubchem.ncbi.nlm.nih.gov/compound/91801202","Name":"Daridorexant","Sub":false}]},{"Name":"Common Chemistry","Urls":[{"Link":"https://commonchemistry.cas.org/detail?cas_rn=1505484-82-1","Name":"Daridorexant","Sub":false}]},{"Name":"UNII","Urls":[{"Link":"https://gsrs.ncats.nih.gov/ginas/app/ui/substances/LMQ24G57E9","Name":"Daridorexant","Sub":false}]},{"Name":"EPA DSSTox","Urls":[{"Link":"https://comptox.epa.gov/dashboard/chemical/details/DTXSID701336356","Name":"Daridorexant","Sub":false}]}],"Refs":["National Center for Biotechnology Information. PubChem Compound Summary for CID 91801202, Daridorexant. Accessed August 10, 2026. \u003ca href=https://pubchem.ncbi.nlm.nih.gov/compound/91801202\u003ehttps://pubchem.ncbi.nlm.nih.gov/compound/91801202\u003c/a\u003e","U.S. Food and Drug Administration; National Center for Advancing Translational Sciences. Daridorexant. UNII: LMQ24G57E9. Global Substance Registration System. Accessed August 10, 2026. \u003ca href=https://gsrs.ncats.nih.gov/ginas/app/beta/substances/LMQ24G57E9\u003ehttps://gsrs.ncats.nih.gov/ginas/app/beta/substances/LMQ24G57E9\u003c/a\u003e","Summary Basis of Decision for Quviviq. August 4, 2023. Accessed August 10, 2026. \u003ca href=https://dhpp.hpfb-dgpsa.ca/review-documents/resource/SBD1691500592141\u003ehttps://dhpp.hpfb-dgpsa.ca/review-documents/resource/SBD1691500592141\u003c/a\u003e","Details for: Quviviq. September 8, 2023. Accessed August 10, 2026. \u003ca href=https://dhpp.hpfb-dgpsa.ca/dhpp/resource/102615\u003ehttps://dhpp.hpfb-dgpsa.ca/dhpp/resource/102615\u003c/a\u003e","Daridorexant Medicinal forms. The National Institute for Health and Care Excellence (NICE). Accessed August 10, 2026. \u003ca href=https://bnf.nice.org.uk/drugs/daridorexant/medicinal-forms/\u003ehttps://bnf.nice.org.uk/drugs/daridorexant/medicinal-forms/\u003c/a\u003e","Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J. Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders. Expert Opinion on Drug Metabolism \u0026 Toxicology. 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