Sitaxentan
Sitaxentan Uses, Dosage, Side Effects, Food Interaction and all others data.
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.
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.
| Trade Name | Sitaxentan |
| Generic | Sitaxentan |
| Sitaxentan Other Names | Sitaxentan, Sitaxsentan |
| Type | |
| Formula | C18H15ClN2O6S2 |
| Weight | Average: 454.905 Monoisotopic: 454.006005309 |
| Protein binding | 99% + |
| Groups | Approved, Investigational, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Investigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure.
How Sitaxentan works
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.
Food Interaction
- Take with or without food.
Elimination Route
70-100%
Half Life
10 hours
Elimination Route
Renal (50 to 60%) Fecal (40 to 50%)
Innovators Monograph
You find simplified version here Sitaxentan
