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... In 2010, Pfizer voluntarily removed sitaxentan from the market over concerns of hepatotoxicity.
- Mechanism
- Curator reviewed
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.
- Primary indication
- Investigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure.Curator reviewed
- Formula / weight
- C18H15ClN2O6S2 · 454.905 g/mol (avg)
- First approval
- Canada, 2008
- Also known as
- Sitaxsentan
- Code names
- IPI-1040 · TBC-11251
Resolves to
PHWXUGHIIBDVKD-UHFFFAOYSA-NSMILESCC1=NOC(NS(=O)(=O)C2=C(SC=C2)C(=O)CC2=CC3=C(OCO3)C=C2C)=C1ClWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Sitaxentan, and which of those have an active Phase 3 trial?
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