darusentan
Small moleculeexperimental
Darusentan is an endothelin receptor antagonist. Gilead Colorado, a subsidiary of Gilead Sciences, under license from Abbott Laboratories, is developing darusentan for the potential treatment of uncontrolled hypertension. — Wikipedia
Clinical trial activity
6 trials · 2 clinical orgs · 0 marketing orgs
Phase 1
0
Phase 2
6
Phase 3
4
Phase 4
0
Earliest trial started Jun 1, 2004 (NCT00364026)
Timeline
Indications
Mechanism of action
- Endothelin receptor ET-AANTAGONIST
EDNRA antagonist
Discontinued failed to meet primary endpoints in phase 3 study
- Endothelin receptor ET-BANTAGONIST
EDNRB antagonist
Discontinued failed to meet primary endpoints in phase 3 study
Chemistry & pharmacology
Loading structure…
SMILES
COc1cc(OC)nc(O[C@H](C(=O)O)C(OC)(c2ccccc2)c2ccccc2)n1- Mol. weight
- 410.43 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaDarusentan ↗
- ChEMBLCHEMBL23261 ↗
Also known as
- 2-(4,6-dimethoxypyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid
- benzenepropanoic acid, alpha-((4,6-dimethoxy-2-pyrimidinyl)oxy)-beta-methoxy-beta-phenyl-, (s)-
- darusentan
- darusentan
- darusentan
- darusentan
- darusentan
- hmr-4005
- hmr-4005
- lu 127043
- lu 135252
- lu-135252
- lu-135252
- lu-135252
- (+)-(s)-2-((4,6-dimethoxy-2-pyrimidinyl)oxy)-3-methoxy-3,3-diphenylpropionic acid
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00738049 | Phase 2 | Jun 1, 2009 | Gilead Sciences, University of Texas at Houston |
| NCT00389675 | Phase 3 | May 1, 2007 | Gilead Sciences |
| NCT00353574 | Phase 3 | Sep 1, 2006 | Gilead Sciences |
| NCT00389779 | Phase 3 | Sep 1, 2006 | Gilead Sciences |
| NCT00330369 | Phase 3 | Jun 1, 2006 | Gilead Sciences |
| NCT00364026 | Phase 2 | Jun 1, 2004 | Gilead Sciences |
Showing 6 of 6 trials
Page 1 / 1
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Gilead Sciences | For profit | 6 | 5 | 2 | 2004 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2009 |
2 organizations
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