Investigational Drug Details
| Drug ID: | D443 |
| Drug Name: | Sitaxentan |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB06268 |
| DrugBank Description: | Sitaxentan was marketed under the trade name Thelin for the treatment of pulmonary arterial hypertension (PAH) by Encysive Pharmaceuticals until Pfizer purchased Encysive in February 2008. In 2010, Pfizer voluntarily removed sitaxentan from the market over concerns of hepatotoxicity. |
| PubChem ID: | 216235 |
| CasNo: | 184036-34-8 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC1=NOC(NS(=O)(=O)C2=C(SC=C2)C(=O)CC2=CC3=C(OCO3)C=C2C)=C1Cl |
| Structure: |
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| InChiKey: | PHWXUGHIIBDVKD-UHFFFAOYSA-N |
| Molecular Weight: | 454.905 |
| DrugBank Targets: | Endothelin-1 receptor; Endothelin B receptor |
| DrugBank MoA: | Sitaxentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, Sitaxentan decreases pulmonary vascular resistance. Sitaxentan has a higher affinity for ET-A than ET-B. |
| DrugBank Pharmacology: | Sitaxentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Sitaxentan blocks the binding of endothelin to its receptors, thereby negating endothelin's deleterious effects. |
| DrugBank Indication: | Investigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure. |
| Targets: | |
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