velusetrag
Small moleculeexperimental
Velusetrag (INN, USAN; previously known as TD-5108) is an experimental drug candidate for the treatment of gastric neuromuscular disorders including gastroparesis, and lower gastrointestinal motility disorders including chronic idiopathic constipation and irritable bowel syndrome. It is a potent, selective, high efficacy 5-HT4 receptor serotonin agonist being developed by Theravance Biopharma and Alfa Wassermann. Velusetrag demonstrates less selectivity for other serotonin receptors, such as 5-HT2 and 5-HT3, to earlier generation 5-HT agonists like cisapride and tegaserod. — Wikipedia
Clinical trial activity
4 trials · 2 clinical orgs · 0 marketing orgs
Phase 1
1
Phase 2
3
Phase 3
0
Phase 4
0
Earliest trial started Oct 1, 2006 (NCT00391820)
Timeline
Indications
Mechanism of action
- Serotonin 4 (5-HT4) receptorAGONIST
HTR4 agonist
Chemistry & pharmacology
Loading structure…
SMILES
CC(C)n1c(=O)c(C(=O)N[C@H]2C[C@H]3CC[C@@H](C2)N3C[C@@H](O)CN(C)S(C)(=O)=O)cc2ccccc21- Mol. weight
- 504.65 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaVelusetrag ↗
- ChEMBLCHEMBL2087337 ↗
Also known as
- 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid ((1s,3r,5r)-8-((r)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl)-8-aza-bicyclo(3.2.1)oct-3-yl)amide
- td5108
- td-5108
- td-5108
- td-5108
- td-5108
- velusetrag
- velusetrag
- velusetrag
- velusetrag
- velusetrag
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02267525 | Phase 2 | Dec 1, 2014 | Alfa Wassermann, Theravance |
| NCT01718938 | Phase 2 | Dec 1, 2012 | Alfa Wassermann, Theravance |
| NCT01467726 | Phase 1 | Nov 1, 2011 | Theravance |
| NCT00391820 | Phase 2 | Oct 1, 2006 | Theravance |
Showing 4 of 4 trials
Page 1 / 1
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Theravance | For profit | 4 | 4 | 2 | 2006 |
| Alfa Wassermann | For profit | 2 | 0 | 1 | 2012 |
2 organizations
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