Pulmonary arterial hypertension (PAH) classified as WHO functional class III

Active Ingredient: Sitaxentan

Indication for Sitaxentan

Population group: only adolescents (12 years - 18 years old) , adults (18 - 65 years old)

Treatment of patients with pulmonary arterial hypertension (PAH) classified as WHO functional class III, to improve exercise capacity. Efficacy has been shown in primary pulmonary hypertension and in pulmonary hypertension associated with connective tissue disease.

For this indication, competent medicine agencies globally authorize below treatments:

100 mg once daily

Route of admnistration


Defined daily dose

100 - 100 mg

Dosage regimen

From 100 To 100 mg once every day

Detailed description

Sitaxentan is to be taken orally as a dose of 100 mg once daily. It may be taken with or without food and without regard to the time of day.

In the case of clinical deterioration despite sitaxentan treatment for at least 12 weeks, alternative therapies should be considered. However, a number of patients who showed no response by week 12 of treatment with sitaxentan responded favourably by week 24, so an additional 12 weeks of treatment may be considered.

Higher doses did not confer additional benefit sufficient to offset the increased risk of adverse reactions, particularly liver injury.

Discontinuation of treatment

There is limited experience with abrupt discontinuation of sitaxentan sodium. No evidence for acute rebound has been observed.

Dosage considerations

It may be taken with or without food and without regard to the time of day.

Active ingredient


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.

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