Review on bosentan, a dual endothelin receptor antagonist for the treatment of pulmonary arterial hypertension

The dual endothelin receptor antagonist, bosentan, is an orally active therapy, which has been proved to be effective in the treatment of pulmonary arterial hypertension (PAH). This review critically addresses and highlights pharmacological aspects of bosentan such as safety, tolerability and drug i...

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Bibliographic Details
Published inRecent patents on cardiovascular drug discovery Vol. 5; no. 3; p. 184
Main Authors Serasli, Eva, Michaelidis, Vassilis, Kosmas, Andreas, Antoniadou, Maria, Tsara, Venetia
Format Journal Article
LanguageEnglish
Published United Arab Emirates 01.11.2010
Subjects
Animals
Antihypertensive Agents - adverse effects
Antihypertensive Agents - pharmacology
Antihypertensive Agents - therapeutic use
Drug Interactions
Endothelin Receptor Antagonists
Humans
Hypertension, Pulmonary - drug therapy
Randomized Controlled Trials as Topic
Sulfonamides - adverse effects
Sulfonamides - pharmacology
Sulfonamides - therapeutic use
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Summary:The dual endothelin receptor antagonist, bosentan, is an orally active therapy, which has been proved to be effective in the treatment of pulmonary arterial hypertension (PAH). This review critically addresses and highlights pharmacological aspects of bosentan such as safety, tolerability and drug interactions. The biological basis of its mode of action is demonstrated in preclinical studies on animal models of PH and an up-to-date review of clinical data is provided, supporting its practical use with a view to achieve optimal treatment goals. Major pivotal randomized placebo-control clinical trials are discussed, together with recently published data concerning its promising role as part of combination therapy. Furthermore, recent patents of novel pharmaceutical interventions in the field of PAH, expanding treatment options, are presented.