Idalopirdine: Difference between revisions
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{{Short description|Chemical compound}} |
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{{Drugbox |
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| IUPAC_name = |
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| IUPAC_name = 2-(6-Fluoro-1''H''-indol-3-yl)-''N''-(3-(2,2,3,3-tetrafluoropropoxy)benzyl)ethanamine |
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| bioavailability = |
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<!--Identifiers--> |
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| CAS_number_Ref = {{cascite|changed|??}} |
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| CAS_number = |
| CAS_number = 467459-31-0 |
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| ATC_prefix = None |
| ATC_prefix = None |
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| PubChem = |
| PubChem = 21071390 |
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| ChEMBL = 3286580 |
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| synonyms = Lu-AE-58054 |
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| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} |
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| ChemSpiderID = 19878969 |
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| KEGG_Ref = {{keggcite|correct|kegg}} |
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| KEGG = D10710 |
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| UNII_Ref = {{fdacite|correct|FDA}} |
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| UNII = 59WCJ0YNWM |
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| smiles = FC(F)C(F)(F)COc1cccc(c1)CNCCc3c[nH]c2cc(F)ccc23 |
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| StdInChI_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChI = 1S/C20H19F5N2O/c21-15-4-5-17-14(11-27-18(17)9-15)6-7-26-10-13-2-1-3-16(8-13)28-12-20(24,25)19(22)23/h1-5,8-9,11,19,26-27H,6-7,10,12H2 |
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| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} |
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| StdInChIKey = YBAWYTYNMZWMMJ-UHFFFAOYSA-N |
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| C=20 | H=19 | F=5 | N=2 | O=1 |
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'''Lu AE58054''' is a [[potency (pharmacology)|potent]] and [[binding selectivity|selective]] [[5-HT6 receptor|5-HT<sub>6</sub> receptor]] [[receptor antagonist|antagonist]] under development by [[Lundbeck]] as an [[augmentation (psychiatry)|augmentation therapy]] for the treatment of [[cognitive deficit]]s associated with [[Alzheimer's disease]] and [[schizophrenia]].<ref name="urlU.S. Development Programs. - Lundbeck">{{cite web | url = http://www.lundbeckinc.com/usa/pipeline/default.asp | title = U.S. Development Programs. |
'''Idalopirdine''' ([[International Nonproprietary Name|INN]]) (code names '''Lu AE58054''',) is a [[potency (pharmacology)|potent]] and [[binding selectivity|selective]] [[5-HT6 receptor|5-HT<sub>6</sub> receptor]] [[receptor antagonist|antagonist]] under development by [[Lundbeck]] as an [[augmentation (psychiatry)|augmentation therapy]] for the treatment of [[cognitive deficit]]s associated with [[Alzheimer's disease]] and [[schizophrenia]].<ref name="urlU.S. Development Programs. - Lundbeck">{{cite web | url = http://www.lundbeckinc.com/usa/pipeline/default.asp | title = U.S. Development Programs. | work = Lundbeck }}</ref><ref name="urlSearch of: Lu AE58054 - List Results - ClinicalTrials.gov">{{cite web | url = http://clinicaltrials.gov/ct2/results?term=Lu+AE58054 | title = Search of: Lu AE58054 - List Results | work = ClinicalTrials.gov | publisher = National Library of Medicine, U.S. Department of Health and Human Services }}</ref> As of October 2013 it is in [[Clinical trial#Phase III|phase III clinical trials]].<ref name="urlSearch of: Lu AE58054 - List Results - ClinicalTrials.gov"/> |
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A phase III trial of two different daily doses of Lu AE58054 on top of 10 mg of [[donepezil]] for mild-to-moderate Alzheimer's failed to meet its [[primary endpoint]] with either dose.<ref name=Taylor-fb>{{cite web | vauthors = Taylor NP | date = 23 September 2016 | url = http://www.fiercebiotech.com/biotech/phiii-alzheimer-s-flop-takes-chunk-out-lundbeck-hits-axovant-aftershocks | title = PhIII Alzheimer's flop takes chunk out of Lundbeck, hits Axovant with aftershocks }}</ref> Two further phase III trials failed too, the company confirmed in early 2017.<ref name=Taylor-fb/> |
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==See also== |
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* [[Cerlapirdine]] |
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* [[Latrepirdine]] |
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==External links== |
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⚫ | * [http://www.lundbeck.com/investor/releases/ReleaseDetails/Release_1272757_EN.asp Lundbeck expands its pipeline - initiating phase II clinical trials with a new compound for the treatment of schizophrenia] {{Webarchive|url=https://web.archive.org/web/20110709031205/http://www.lundbeck.com/investor/releases/ReleaseDetails/Release_1272757_EN.asp |date=2011-07-09 }} |
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⚫ | * [http://www.lundbeck.com/investor/releases/ReleaseDetails/Release_1357623_EN.asp Lundbeck initiates clinical phase II trials with Lu AE58054 as augmentation treatment in Alzheimer's disease] {{Webarchive|url=https://web.archive.org/web/20100204055707/http://lundbeck.com/investor/releases/ReleaseDetails/Release_1357623_EN.asp |date=2010-02-04 }} |
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{{Antidementia}} |
{{Antidementia}} |
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{{Nootropics}} |
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{{Serotonergics}} |
{{Serotonergics}} |
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{{Tryptamines}} |
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[[Category:5-HT6 antagonists]] |
[[Category:5-HT6 antagonists]] |
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[[Category:Antidementia agents]] |
[[Category:Antidementia agents]] |
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[[Category:Nootropics]] |
[[Category:Nootropics]] |
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[[Category:Tryptamines]] |
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[[Category:Organofluorides]] |
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[[Category:Fluoroarenes]] |