Bosentan
Encyclopedia
Bosentan is a dual endothelin receptor antagonist
used in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States
, the European Union
and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.
-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, bosentan decreases pulmonary vascular resistance. Bosentan has a slightly higher affinity for ET-A than ET-B.
In the United States, bosentan is indicated for the treatment of pulmonary arterial hypertension (WHO Group I) in patients with WHO Class II-IV symptoms, to improve exercise capacity and decrease the rate of clinical worsening.
Bosentan use requires hematocrit monitoring due to potential onset of anemia.
Hormone-based contraception is not possible in women taking Bosentan, due to a pharmacokinetic interaction.
Bosentan is absolutely contraindicated in pregnancy because of its teratogenicity. Category X.
Endothelin receptor antagonist
A endothelin receptor antagonist is a drug that blocks endothelin receptors.Three main kinds of ERAs exist:* selective ETA receptor antagonists , which affect endothelin A receptors....
used in the treatment of pulmonary artery hypertension (PAH). It is licensed in the United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
, the European Union
European Union
The European Union is an economic and political union of 27 independent member states which are located primarily in Europe. The EU traces its origins from the European Coal and Steel Community and the European Economic Community , formed by six countries in 1958...
and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer.
Mechanism of action
Bosentan is a competitive antagonist of endothelinEndothelin
Endothelins are proteins that constrict blood vessels and raise blood pressure. They are normally kept in balance by other mechanisms, but when they are over-expressed, they contribute to high blood pressure and heart disease....
-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, bosentan decreases pulmonary vascular resistance. Bosentan has a slightly higher affinity for ET-A than ET-B.
Clinical uses
Bosentan is indicated mainly for the treatment of pulmonary hypertension. In 2007, bosentan was approved in the European Union also for reducing the number of new digital ulcers in patients with systemic sclerosis and ongoing digital ulcer disease.In the United States, bosentan is indicated for the treatment of pulmonary arterial hypertension (WHO Group I) in patients with WHO Class II-IV symptoms, to improve exercise capacity and decrease the rate of clinical worsening.
Warnings
Due to potential hepatotoxicity, the FDA requires monthly monitoring of liver function tests while taking Bosentan.Bosentan use requires hematocrit monitoring due to potential onset of anemia.
Hormone-based contraception is not possible in women taking Bosentan, due to a pharmacokinetic interaction.
Bosentan is absolutely contraindicated in pregnancy because of its teratogenicity. Category X.