Chemical formula: C₁₈H₁₅ClN₂O₆S₂ Molecular mass: 454.905 g/mol PubChem compound: 216235
Sitaxentan is a potent (Ki 0.43 nM) and highly selective ETA antagonist (approximately 6,500-fold more selective for ETA as compared to ETB). Endothelin-1 (ET-1) is a potent vascular paracrine and autocrine peptide in the lung, and can also promote fibrosis, cell proliferation, cardiac hypertrophy, and remodelling and is pro-inflammatory. ET-1 actions are mediated through endothelin A (ETA) and endothelin B receptors (ETB). ET-1 concentrations are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension (PAH), as well as other cardiovascular disorders and connective tissue diseases.
This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:
| ATC code | Group title | Classification |
|---|---|---|
| C02KX03 | Sitaxentan | C Cardiovascular system → C02 Antihypertensives → C02K Other antihypertensives → C02KX Antihypertensives for pulmonary arterial hypertension |
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
| Title | Information Source | Document Type | |
|---|---|---|---|
| THELIN Film-coated tablet | European Medicines Agency (EU) | MPI, EU: SmPC |
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