Medicines
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Discover all available medicines and treatments
Brand: Thelin
Sitaxsentan is an endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group I) to improve exercise capacity and to delay clinical worsening. It is classified as a dual endothelin receptor antagonist, meaning it blocks the action of endothelin-1, a potent vasoconstrictor and smooth muscle mitogen, at both ETA and ETB receptors. This action helps to reduce pulmonary vascular resistance and improve blood flow in the lungs.
For the treatment of pulmonary arterial hypertension (PAH) to improve exercise capacity and delay clinical worsening.
Sitaxsentan can cause liver injury, including liver failure, which can be fatal. Liver function tests should be performed before starting sitaxsentan and monthly thereafter. Patients should be monitored for signs and symptoms of liver injury.
Outcome:
Increased sitaxsentan levels
Mechanism:
Inhibition of CYP3A4
Outcome:
Increased simvastatin levels
Mechanism:
CYP3A4 inhibition
Outcome:
May slightly decrease absorption
Mechanism:
Unknown
Most likely new formulation: Extended-release formulation (Year: 2026, 60% confidence)
Based on current usage trends and clinical trial data, there is a low likelihood (<5%) of sitaxsentan being withdrawn from the market for safety reasons in the next 5 years.
Endothelin Receptor Antagonist
Sulfonamide