Prostacyclin (IP) receptor agonism
Prostacyclin binds the prostacyclin receptor (IP) located on the surface of platelets and vascular smooth muscle cells. The IP receptor is a G-protein coupled receptor that, upon activation by prostacyclin, stimulates the formation of cyclic adenosine monophosphate (cAMP). Prostacyclin counteracts the vasoconstrictor and pro-thrombotic activity of endothelin.
Actelion is developing an orally available and long-acting non-prostanoid IP receptor agonist that mimics the actions of endogenous prostacyclin for the treatment of PAH.











