INTRODUCTION: Selexipag is a first-in-class orally available selective 
non-prostanoid IP receptor agonist. This review was based on a PubMed search and 
focuses on the potential role of selexipag in the treatment of pulmonary 
arterial hypertension (PAH).
AREAS COVERED: Selexipag is rapidly hydrolyzed to an active metabolite, 
ACT-333679. Both selexipag and its metabolite are highly selective for the IP 
receptor compared with other prostanoid receptors. This selectivity for the IP 
receptor offers the potential for improved tolerability with selexipag, as side 
effects (e.g., nausea and vomiting) that might result from activation of the 
other prostanoid receptors may be minimized. In addition, the selexipag 
metabolite has a half-life of 7.9 h, thus permitting oral dosing twice daily. 
Selexipag showed effects on pharmacodynamic end points obtained with right heart 
catheterization in a Phase II trial in patients with PAH, and is being evaluated 
in the ongoing Phase III trial (GRIPHON trial, Clinicaltrials.gov NCT01106014).
EXPERT OPINION: The signal of a beneficial effect of selexipag on disease 
progression may become more robust for long term under prolonged exposure. 
Pending the GRIPHON trial results, selexipag could provide a convenient 
first-line prostacyclin treatment option for patients with PAH.