Endothelin Antagonism with Bosentan: Current Status and Future Perspectives

ABSTRACT Endothelin receptor antagonist have been proposed for the treatment of a variety of disorders in which the endothelins may act as pathogenic mediators, such as hypertension, congestive heart failure, and cerebral vasospasm. Bosentan is a nonpeptide competitive antagonist, which can be a good tool for studying the endothelin system. It is specific for the endothelin system and blocks the actions of endothelin at both mammalian receptors (A and B). Bosentan has recently moved into Phase III clinical trial. This review will attempt to overview the experimental and clinical effects of bosentan. SUMMARY ET receptor antagonists, such as bosentan, produce beneficial effects in various pathological conditions. Bosentan, as a mixed ET A /ET B receptor antagonist, may be of particular benefit in heart failure and cerebral vasospasm where ET B receptors are upregulated. For some clinical indications bosentan should be evaluated more vigorously in further controlled clinical trials.