sitaxentan
Small moleculeexperimental
Sitaxentan sodium (TBC-11251) is a medication for the treatment of pulmonary arterial hypertension (PAH). It was marketed as Thelin by Encysive Pharmaceuticals until Pfizer purchased Encysive in February 2008. In 2010, Pfizer voluntarily removed sitaxentan from the market due to concerns about liver toxicity. — Wikipedia
Clinical trial activity
18 trials · 5 clinical orgs · 0 marketing orgs
Phase 1
5
Phase 2
12
Phase 3
8
Phase 4
0
Earliest trial started Apr 24, 2002 (NCT00034307)
Timeline
Indications
Studied for
- Asthma · Phase 2
- Blood Pressure · Phase 2
- General Surgery · Phase 2
- Healthy Volunteers · Phase 1
- Heart Failure, Diastolic · Phase 2
- Heart Valve Diseases · Phase 2
- Hypertension, Pulmonary · Phase 3
- Lung Diseases · Phase 2
- Proteinuria · Phase 2
- Pulmonary Arterial Hypertension · Phase 3
- Renal Insufficiency, Chronic · Phase 2
- Vasoconstriction · Early Phase 1
- Vasodilation · Early Phase 1
Mechanism of action
- Endothelin receptor ET-AANTAGONIST
EDNRA antagonist
Chemistry & pharmacology
Loading structure…
SMILES
Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2- Mol. weight
- 454.91 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL282724 ↗
- WikipediaSitaxentan ↗
- ChEMBLCHEMBL2105740 ↗
Also known as
- n-(4-chloro-3-methyl-5-isoxazolyl)-2-(3,4-(methylenedioxy)-6-methyl)phenylacetyl-3-thiophenesulfonamide
- n-(4-chloro-3-methyl-5-isoxazolyl)-2-((4,5-(methylenedioxy)-o-toly)acetyl)-3-thiophenesulfonamide
- sitaxentan
- sitaxentan
- sitaxentan
- sitaxentan
- sitaxentan
- sitaxentan
- sitaxentan
- sitaxentan
- sitaxentan sodium
- sitaxentan sodium
- sitaxentan sodium
- sitaxentan sodium
- sitaxsentan
- sitaxsentan
- sitaxsentan
- sitaxsentan
- sitaxsentan
- sitaxsentan sodium
- sitaxsentan sodium
- sitaxsentan sodium
- tbc11251
- tbc11251
- tbc 11251
- tbc-11251
- tbc-11251
- tbc-11251na
- tbc-11251na
- tbc-11251z
- tbc-11251z
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01251848 | Phase 1 | Jan 1, 2011 | Pfizer |
| NCT01251835 | Phase 1 | Dec 1, 2010 | Pfizer |
| NCT01244620 | Phase 1 | Nov 1, 2010 | Pfizer |
| NCT01210443 | Phase 3 | Nov 1, 2010 | Pfizer |
| NCT01204853 | Phase 3 | Aug 1, 2010 | Pfizer |
| NCT00796510 | Phase 3 | Jul 1, 2010 | Pfizer |
| NCT01050491 | Phase 2 | Nov 1, 2009 | Institut National de la Santé Et de la Recherche Médicale, France |
| NCT00981968 | Phase 1 | Sep 1, 2009 | Pfizer |
| NCT00796666 | Phase 3 | May 1, 2009 | Pfizer |
| NCT01100736 | Early Phase 1 (Phase 1) | Jan 1, 2009 | Encysive, University of Edinburgh |
| NCT00795639 | Phase 3 | Dec 1, 2008 | Pfizer |
| NCT00817037 | Phase 2 | May 1, 2007 | Encysive, University of Edinburgh |
| NCT00810732 | Phase 2 | May 1, 2007 | Pfizer |
| NCT00838383 | Phase 2 | Aug 1, 2006 | Pfizer |
| NCT00303498 | Phase 2 | Mar 1, 2006 | Pfizer |
| NCT00080457 | Phase 3 | May 1, 2003 | Encysive |
| NCT00811018 | Phase 3 | Mar 1, 2003 | Pfizer |
| NCT00034307 | Phase 2/Phase 3 (Phase 3) | Apr 24, 2002 | Encysive, ICOS |
Showing 18 of 18 trials
Page 1 / 1
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 13 | 13 | 3 | 2003 |
| Encysive | For profit | 4 | 1 | 3 | 2002 |
| University of Edinburgh | Academic/Hospital | 2 | 2 | 2 | 2007 |
| ICOS | For profit | 1 | 1 | 1 | 2002 |
| Institut National de la Santé Et de la Recherche Médicale, France | Academic/Hospital | 1 | 1 | 1 | 2009 |
5 organizations
Page 1 / 1