About Actelion's PGI2 Receptor Agonist

ACT-293987, originally discovered and synthesized by Nippon Shinyaku, is a long-lasting orally available prodrug of the active principle, a potent non-prostanoid PGI2 receptor agonist, which exerts vasodilating effects. ACT-293987 has major potential as a novel treatment of pulmonary arterial hypertension.

In April 2008, Actelion and Nippon Shinyaku signed a licensing agreement, by which Actelion will be responsible for global development and commercialization of ACT-293987 outside Japan, whereas the two companies will co-develop and co-commercialize in Japan.

Current Status

Nippon Shinyaku has recently completed a phase I study in the United Kingdom. A phase IIa study in PAH patients has been initiated in Europe, with the objective to evaluate acute hemodynamic effects and tolerability of up-titration to 800µg bid.

Supporting Studies

Data from the Phase I study indicated that multiple doses up to 600 µg bid were well tolerated. There was no clinically relevant pharmacokinetic, pharmacodynamic interaction with warfarin.