tezosentan
Small moleculeexperimental
Tezosentan is a non-selective ETA and ETB receptor antagonist. It acts as a vasodilator and was designed by Actelion as a therapy for patients with acute heart failure. However, studies showed that tezosentan did not improve dyspnea or reduce the risk of fatal or nonfatal cardiovascular events. — Wikipedia
Clinical trial activity
5 trials · 7 clinical orgs · 0 marketing orgs
Phase 1
0
Phase 2
5
Phase 3
3
Phase 4
0
Earliest trial started Apr 1, 2003 (NCT00524433)
Timeline
Indications
Mechanism of action
- Endothelin receptor ET-AANTAGONIST
EDNRA antagonist
Discontinueddue to lack of clinical benefit.
- Endothelin receptor ET-BANTAGONIST
EDNRB antagonist
Discontinueddue to lack of clinical benefit.
Chemistry & pharmacology
Loading structure…
SMILES
COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C(C)C)cn2)nc(-c2ccnc(-c3nnn[nH]3)c2)nc1OCCO- Mol. weight
- 605.64 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTezosentan ↗
- ChEMBLCHEMBL61780 ↗
Also known as
- 5-isopropyl-pyridine-2-sulfonic acid 6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-1h-tetrazol-5-yl--pyridin-4-yl)--pyrimidin-4-ylamide
- act-050089
- act-050089
- act-050089
- ro 610612
- ro 61-0612
- ro-610612
- ro-610612
- ro-61-0612
- ro-61-0612
- tezosentan
- tezosentan
- tezosentan
- tezosentan
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01094067 | Phase 2 | Sep 1, 2010 | Actelion |
| NCT01077297 | Phase 2 | Aug 1, 2010 | Actelion |
| NCT00458276 | Phase 3 | Apr 1, 2007 | Actelion, Papworth Hospital NHS Foundation Trust, Stanford University, University of Montreal, University of Pavia, University of Vienna, Yeshiva University |
| NCT00524433 | Phase 3 | Apr 1, 2003 | Actelion |
| NCT00525707 | Phase 3 | Apr 1, 2003 | Actelion |
Showing 5 of 5 trials
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Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Actelion | For profit | 5 | 5 | 2 | 2003 |
| Papworth Hospital NHS Foundation Trust | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Stanford University | Academic/Hospital | 1 | 0 | 1 | 2007 |
| University of Montreal | Academic/Hospital | 1 | 0 | 1 | 2007 |
| University of Pavia | Academic/Hospital | 1 | 0 | 1 | 2007 |
| University of Vienna | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Yeshiva University | Academic/Hospital | 1 | 0 | 1 | 2007 |
7 organizations
Page 1 / 1