We have the exclusive right to develop and market a modified release formulation
of beraprost (beraprost-MR) in the United States, Canada, Mexico, South America,
Europe, Egypt, India, South Africa and Australia for the treatment of cardiovascular
indications, pursuant to our license agreement with Toray Industries, Inc. Beraprost
is a chemically stable, orally bioavailable prostacyclin analogue. Like natural
prostacyclin and Remodulin, beraprost is believed to dilate blood vessels, prevent
platelet aggregation and prevent proliferation of smooth muscle cells surrounding
blood vessels. In 2007, Toray announced that beraprost-MR received regulatory approval
in Japan for use in the treatment of PAH.
In November 2011, we announced that a phase II trial of beraprost-MR did not provide
data supporting the initiation of a phase III study using a twice daily dosing regimen.
The results of this study suggested that the efficacy of beraprost may be improved
by providing more stable and consistent plasma concentrations of beraprost, thereby
increasing the therapeutic exposure to the drug. Therefore, we commenced studies
of a reformulated, single isomer version of beraprost (314d), with a dosing regimen
of four times per day. We completed a phase I safety trial in July 2012, and the
preliminary data suggests that dosing 314d four times a day is safe. We believe
that 314d and treprostinil bind selectively to different sets of prostacyclin receptors
within the lung and thus could provide certain groups of patients a differing set
of safety and efficacy profiles. We have commenced a phase III study to evaluate
the clinical benefit of 314d as an add-on therapy to Tyvaso® Inhalation Solution.
During the third quarter of 2012, we initiated efforts to develop an extended release
injection we refer to as TransCon Beraprost, which incorporates the TransCon technology
described above and is intended to be self-administered by PAH patients once daily.
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