Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: does selectivity matter?

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 (ET(A) and ET(B)), 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,

SUBMITTER: Opitz CF 

PROVIDER: S-EPMC2515885 | biostudies-literature | 2008 Aug

REPOSITORIES: biostudies-literature