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Therapeutic Focus: Prostacyclin

Eicosanoids represent a diverse family of lipid mediators with fundamental roles in physiology and disease, including vasodilation and vasoconstriction, inflammation, blood clotting, fever, and pain. Our focus on prostacyclin analogues is based on the robust history and research establishing prostacyclin (PGI2), a prostaglandin member of the eicosanoid family of lipid molecules, as a potent inhibitor of platelet aggregation and vasoconstriction that possesses antiproliferative and anti-inflammatory properties. The published data demonstrate that targeting the prostacyclin (IP) receptor can reverse vasoconstriction and enhance cutaneous blood flow, reduce microvascular inflammation, reduce fibrosis, and decrease platelet activation making it relevant for numerous diseases.

Iloprost is a stable analogue of PGI2 and a potent prostacyclin (IP) receptor agonist that reverses vasoconstriction and inhibits platelet activation and fibrosis. Iloprost stimulates generation of cAMP by binding to the IP receptor, thereby affecting phospholipase activity and cytosolic calcium levels in platelets, fibroblasts, and endothelial cells.