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Bosentan, sold under the brand name Tracleer among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery hypertension (PAH). [4] [5] Bosentan is available as film-coated tablets (62.5 mg or 125 mg) or as dispersable tablets for oral suspension (32 mg).
- C₂₇H₂₉N₅O₆S
- Tracleer, Stayveer
- AU: X (High risk), X
- Liver
An endothelin receptor antagonist ( ERA) is a drug that blocks endothelin receptors . Three main kinds of ERAs exist: selective ET A receptor antagonists ( sitaxentan, ambrisentan, atrasentan, BQ-123, sparsentan, zibotentan, avosentan, edonentan, aprocitentan, clazosentan ), which affect endothelin A receptors.
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Is bosentan a dual endothelin receptor antagonist?
What is the difference between bosentan and macitentan?
What is bosentan used for?
What is the bioavailability of bosentan?
Macitentan, sold under the brand name Opsumit, is an endothelin receptor antagonist (ERA) developed by Actelion and approved for the treatment of pulmonary arterial hypertension (PAH). [4] . The other two ERAs marketed as of 2014 are bosentan and ambrisentan. [4] .
- C₁₉H₂₀Br₂N₆O₄S
- AU: X (High risk)
- 588.28 g·mol−1
- Opsumit
Contents. hide. (Top) References. Tezosentan is a non-selective ET A and ET B receptor antagonist. [1] . It acts as a vasodilator and was designed by Actelion as a therapy for patients with acute heart failure. However, studies showed that tezosentan did not improve dyspnea or reduce the risk of fatal or nonfatal cardiovascular events. [2]
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- 605.624 g·mol−1
- C₂₇H₂₇N₉O₆S
- 180384-57-0
Ambrisentan, sold under the brand name Letairis among others, is a drug used for the treatment of pulmonary hypertension. [3] [5] It is an endothelin receptor antagonist. The peptide endothelin constricts muscles in blood vessels, increasing blood pressure.
- C₂₂H₂₂N₂O₄
- Oral
- AU: X (High risk)
- Letairis, Volibris, Pulmonext
Aprocitentan is a dual endothelin-1 antagonist that targets both endothelin A and endothelin B receptors. [3] [4] Aprocitentan was approved for medical use in the United States in March 2024. [1] [2] [5] It is the first endothelin receptor antagonist to be approved by the US Food and Drug Administration (FDA) to treat systemic hypertension. [2]
Busulfan ( Myleran, GlaxoSmithKline, Busulfex IV, Otsuka America Pharmaceutical, Inc.) is a chemotherapy drug in use since 1959. It is a cell cycle non-specific alkylating antineoplastic agent, in the class of alkyl sulfonates. Its chemical designation is 1,4-butanediol dimethanesulfonate. History.
