almorexant
Small moleculeexperimental
Almorexant (INN), also known by its development code ACT-078573, is an orexin antagonist, acting as a competitive antagonist of the OX1 and OX2 orexin receptors, which was being developed by the pharmaceutical companies Actelion and GSK for the treatment of insomnia. Development of the drug was abandoned in January 2011 due to concerns over the hepatic safety of almorexant after transient increases in liver enzymes were observed in trials. — Wikipedia
Clinical trial activity
6 trials · 6 clinical orgs · 0 marketing orgs
Phase 1
3
Phase 2
2
Phase 3
1
Phase 4
0
Earliest trial started May 1, 2006 (NCT00640848)
Timeline
Indications
Mechanism of action
- Orexin receptorANTAGONIST
Orexin receptor antagonist
Chemistry & pharmacology
Loading structure…
SMILES
CNC(=O)[C@@H](c1ccccc1)N1CCc2cc(OC)c(OC)cc2[C@@H]1CCc1ccc(C(F)(F)F)cc1- Mol. weight
- 512.57 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaAlmorexant ↗
- ChEMBLCHEMBL455136 ↗
Also known as
- ((2r)-2-((1s)-6,7-dimethoxy-1-(2-(4-trifluoromethylphenyl)-ethyl)-3,4-dihydro-1h-isoquinolin-2-yl)-n-methyl-2-phenylacetamide)
- act-078573
- act-078573
- act-078573
- almorexant
- almorexant
- almorexant
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01954589 | Phase 1 | Nov 1, 2011 | Actelion |
| NCT01243060 | N/A | May 1, 2011 | Northern California Institute of Research and Education, United States Army |
| NCT01987739 | Phase 1 | Sep 1, 2009 | Kendle International Inc., Midnight Pharma, LLC |
| NCT00608985 | Phase 3 | Mar 1, 2008 | Midnight Pharma, LLC, University of Brussels |
| NCT00606593 | Phase 2 | Dec 1, 2007 | Midnight Pharma, LLC |
| NCT00640848 | Phase 1 | May 1, 2006 | Actelion, Midnight Pharma, LLC |
Showing 6 of 6 trials
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Organizations
Research & Development (6)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Midnight Pharma, LLC | For profit | 4 | 4 | 3 | 2006 |
| Actelion | For profit | 2 | 1 | 1 | 2006 |
| Kendle International Inc. | For profit | 1 | 0 | 1 | 2009 |
| Northern California Institute of Research and Education | Academic/Hospital | 1 | 1 | 1 | 2011 |
| United States Army | Government | 1 | 0 | 1 | 2011 |
| University of Brussels | Academic/Hospital | 1 | 0 | 1 | 2008 |
6 organizations
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