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Drug that blocks endothelin receptors
An endothelin receptor antagonist (ERA ) is a
drug that blocks
endothelin receptors .
Three main kinds of ERAs exist:
selective ETA receptor antagonists (
sitaxentan ,
ambrisentan ,
atrasentan ,
BQ-123 ,
sparsentan ,
zibotentan ,
avosentan ,
edonentan ,
aprocitentan ,
clazosentan ), which affect
endothelin A receptors .
dual antagonists (
bosentan ,
macitentan ,
tezosentan ), which affect both
endothelin A and
B receptors .
[1]
selective ETB receptor antagonists (
BQ-788 and
A192621 ) which affect
endothelin B receptors are used in research but have not yet reached the clinical trial stage.
Macitentan ,
ambrisentan and
bosentan are mainly used for the treatment of
pulmonary arterial hypertension , while
atrasentan is an experimental anti-
cancer drug.
References