Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe (d)

Austria: Thelin; Bulgaria: Thelin; Czech Republic: Thelin; Denmark: Thelin; Estonia: Thelin; Finland: Thelin; France: Thelin; Germany: Thelin; Greece: Thelin; Hungary: Thelin; Ireland: Thelin; Italy: Thelin; Latvia: Thelin; Lithuania: Thelin; Luxembourg: Thelin; Malta: Thelin; Poland: Thelin; Portugal: Thelin; Romania: Thelin; Slovakia: Thelin; Slovenia: Thelin; Sweden: Thelin; UK: Thelin.

North America (d)

Canada: Thelin.

Drug combinations


Sitaxentan: C~18~H~15~ClN~2~O~6~S~2~. Mw: 454.90. N-(4-Chloro-3-methyl-5-isoxazolyl)-2-[[4,5-(methylenedioxy)-o-toly]acetyl]-3-thiophenesulfonamide. CAS-184036-34-8.

Pharmacologic Category

Hypotensive Agents, Miscellaneous; Endothelin Antagonist. Vasodilator. (ATC-Code: C02KX03).

Mechanism of action

A selective antagonist of A subtype of endothelin-1 receptors (ET~A~) located in pulmonary smooth muscle. Stimulation of these receptors by endogenous endothelin-1 causes vasoconstriction. Sitaxsentan exhibits 6500-fold greater selectivity for ET~A~ over the ET~B~ subtype; the latter predominates on vascular endothelial cells. Thus, preferential antagonism of ET~A~ reduces vasoconstriction, without compromising vasodilatory/antiproliferative actions mediated through endothelin-1 binding to ET~B~ subtype.

Therapeutic use

Primary pulmonary arterial hypertension or pulmonary hypertension secondary to connective tissue disease.

Pregnancy and lactiation implications

Use of sitaxsentan contraindicated in pregnancy and lactation.

Unlabeled use


Hypersensitivity to sitaxsentan or any component of the formulation. Concurrent use with cyclosporine. Prior hepatic impairment. Elevated AST/ALT >3 times ULN. Breast-feeding. Pregnancy.

Warnings and precautions

Reduction in hematocrit/hemoglobin may be observed within first few weeks of therapy, with subsequent stabilization of levels observed by week four. Use associated with reversible, dose-dependent transaminase (ALT or AST) elevations. Increased bilirubin levels may also be observed. Mild-to-severe hepatitis (including one fatality) reported with use. Initiate therapy with caution in systemic systolic blood pressure <85 mm Hg. Concurrent use of sitaxsentan with cyclosporine contraindicated. Reduction in warfarin dosing may be necessary when used concurrently with sitaxsentan due to increased risk of prolonged PT/INR.



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