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词条 Idalopirdine
释义

  1. See also

  2. References

  3. External links

{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 451553711
| IUPAC_name = 2-(6-Fluoro-1H-indol-3-yl)-N-(3-(2,2,3,3-tetrafluoropropoxy)benzyl)ethanamine
| image = Lu-AE58054.svg
| tradename =
| pregnancy_category =
| legal_status =
| routes_of_administration =
| bioavailability =
| metabolism =
| elimination_half-life =
| excretion =
| CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 467459-31-0
| ATC_prefix = None
| ATC_suffix =
| PubChem =
| ChEMBL = 3286580
| synonyms = Lu-AE-58054
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 19878969
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D10710
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 59WCJ0YNWM
| smiles = FC(F)C(F)(F)COc1cccc(c1)CNCCc3c[nH]c2cc(F)ccc23
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| 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
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = YBAWYTYNMZWMMJ-UHFFFAOYSA-N
| C=20 | H=19 | F=5 | N=2 | O=1
| molecular_weight = 398.37 g/mol
}}Idalopirdine (INN) (code names Lu AE58054,) is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.[1][2] As of October 2013 it is in phase III clinical trials.[3]

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.[4] Two further phase III trials failed too, the company confirmed in early 2017.[4]

See also

  • Cerlapirdine
  • Latrepirdine

References

1. ^{{cite web | url = http://www.lundbeckinc.com/usa/pipeline/default.asp | title = U.S. Development Programs. - Lundbeck | format = | work = | accessdate = }}
2. ^{{cite web | url = http://clinicaltrials.gov/ct2/results?term=Lu+AE58054 | title = Search of: Lu AE58054 - List Results - ClinicalTrials.gov | format = | work = | accessdate = }}
3. ^{{cite web | url = http://clinicaltrials.gov/ct2/results?term=Lu+AE58054 | title = Search of: Lu AE58054 - List Results - ClinicalTrials.gov | format = | work = | accessdate = }}
4. ^PhIII Alzheimer’s flop takes chunk out of Lundbeck, hits Axovant with aftershocks Sept 2016

External links

  • Lundbeck expands its pipeline - initiating phase II clinical trials with a new compound for the treatment of schizophrenia
  • Lundbeck initiates clinical phase II trials with Lu AE58054 as augmentation treatment in Alzheimer's disease
{{Antidementia}}{{Nootropics}}{{Serotonergics}}

6 : 5-HT6 antagonists|Antidementia agents|Nootropics|Tryptamines|Organofluorides|Fluoroarenes

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