| Item |
Information |
|
Drug Groups
|
approved; investigational |
| Indication |
Investigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure. |
| 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. |
| Biotransformation |
Hepatic (CYP2C9- and CYP3A4-mediated) |
| Absorption |
70-100% |
| Half Life |
10 hours |
| Protein Binding |
99% + |
| Elimination |
Renal (50 to 60%)
Fecal (40 to 50%) |
| External Links |
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