Beraprost (United Therapeutics/Astellas/Kaken Pharmaceutical Co) is an oral chemically stable prostacyclin analog targeting the prostaglandin I2 (PGI2) receptor. PGI2 agonists are potent vasodilators and platelet aggregation inhibitors, and also help to relax smooth muscle cells through counteracting the effect of vasoconstrictive mediators. In pulmonary arterial hypertension, the production of naturally occurring PGI2 is chronically impaired. This plays a crucial role in the excessive vasoconstriction, pulmonary vasculature remodeling, and thrombosis formation associated with the disease pathology.
Beraprost has been reformulated to ensure that the drug demonstrates sustained clinical efficacy. In November 2011, United Therapeutics announced that Phase II data for a modified-release version of beraprost, beraprost-MR, did not support the initiation of a Phase III study. This led to the development of a reformulated single isomer version of beraprost, known as beraprost 314d. Beraprost 314d is dosed four times daily versus beraprost-MR’s twice-daily dosing.
While there is high demand within pulmonary arterial hypertension (PAH) for an oral prostanoid therapy, beraprost’s continual reformulations raise questions over its sustained clinical efficacy. United Therapeutics is currently developing a reformulated single isomer version of beraprost as an add-on therapy to the inhaled prostanoid therapy Tyvaso (treprostinil; United Therapeutics). As such, Datamonitor Healthcare believes that beraprost 314d’s anticipated commercial potential is limited by questions over its efficacy and small target patient population.
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