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%)

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