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• W2122242529 endingPage "1948" @default.
• W2122242529 startingPage "1936" @default.
• W2122242529 abstract "Treatment options for pulmonary arterial hypertension (PAH) have considerably improved in the past few years. Endothelin (ET)-receptor antagonism has been established as a first-line option for the majority of PAH patients. Endothelin-receptor antagonists (ETRAs) comprise sulfonamide and non-sulfonamide agents with different affinities for ET-receptor subtypes (ETA and ETB), and the focus of development has shifted from drugs with less selectivity to those with high selectivity. There is ongoing debate as to whether selective or non-selective ET-receptor antagonism is more beneficial in the treatment of PAH. This paper reviews the current evidence from experimental and clinical studies obtained from a thorough literature search focusing on the three marketed drugs bosentan, sitaxentan, and ambrisentan. A clinically meaningful difference among the three approved ETRAs with respect to their ET-receptor selectivity could not be demonstrated to date. Therefore, in clinical practice, other features are likely to be of greater relevance when considering treatment, such as the potential for serious drug–drug interactions, convenience of dosing schedule, or rates of limiting side effects. These characteristics bear more relation to the chemical or pharmacological properties of the drugs than to receptor selectivity itself." @default.
• W2122242529 created "2016-06-24" @default.
• W2122242529 creator A5014869966 @default.
• W2122242529 creator A5025740262 @default.
• W2122242529 creator A5026155358 @default.
• W2122242529 creator A5053155088 @default.
• W2122242529 date "2008-06-17" @default.
• W2122242529 modified "2023-09-23" @default.
• W2122242529 title "Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: does selectivity matter?" @default.
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• W2122242529 doi "https://doi.org/10.1093/eurheartj/ehn234" @default.

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