Treprostinil is a stable tricyclic analogue of prostacyclin, it promotes vasodilation and inhibition of platelet aggregation. Treprostinil is administered either subcutaneously, orally or through inhalation used to treat pulmonary arterial hypertension as it acts as an anti-thrombotic agent and potent vasodilator. The drug binds and activates prostacyclin, prostaglandin D2 and P2Y purinoceptor 12 receptors that lead to activation and increased formation of cAMP levels. These elevated cAMP concentrations cause the efflux of calcium and calcium-activated potassium channels leading to cell hyperpolarization. Leading to the inhibition of platelet aggregation and vasodilation of the blood vessels. Treprostinil is metabolized by the liver by CYP2C8 and CYP2C into other metabolites that are excreted in urine.

Treprostinil Pathway References