ACT-333679

ACT-333679 is the pharmacologically active metabolite of selexipag, a selective prostacyclin (IP) receptor agonist. It is approximately 37-fold more potent than selexipag and mediates most of the clinical effects of selexipag by binding selectively to the prostacyclin IP receptor. This activation leads to vasodilation, inhibition of cell proliferation, and prevention of platelet aggregation, effects that are beneficial in treating pulmonary arterial hypertension. ACT-333679 has also shown potential antifibrotic activity by inhibiting Erk1/2 and Akt phosphorylation in fibroblasts in vitro. It is produced in vivo following oral administration of selexipag, via hydrolysis by carboxylesterases, and has a terminal half-life of about 6–13.5 hours[1][3][4].

Other names

MRE-269MRE269MRE 269