Nitric oxide pathway
- Nitric oxide pathway
- Phosphodiesterase type 5 inhibitors (PDE5is)1
- Soluble guanylate cyclase (sGC) stimulator1
- Endothelin pathway
- Endothelin receptor antagonists (ERAs)1
- Anti-proliferation
- Treatment effect3,4
- Vasodilation
- Anti-proliferation
- Treatment effect5
- Vasodilation
- Prostacyclin pathway
- Prostacyclin (IP) receptor agonist
- Selexipag has a chemical structure unrelated to prostacyclin and its analogs1,6
- Highly selective activation of the target IP receptor1,6
- Prostacyclin analogs2
- Epoprostenol
- Treprostinil
- Iloprost
- Prostacyclin analogs activate at least 1 prostanoid receptor in addition to IP1
- Treatment effect1,3
- Vasodilation
- Anti-proliferation
- Anti-inflammatory
- Anti-thrombotic
- Pulmonary artery
Focusing on targeting the 3 foundational pathways in PAH is an effective treatment strategy with clinical benefits2
Not all prostacyclin pathway agents are the same.1 UPTRAVI® selectively targets the IP receptor—the only established relaxant prostanoid receptor in the human pulmonary artery6,7
Three established prostanoid receptors in the human pulmonary artery7
Animal studies have shown":
Promotes vasodilation and antiproliferation7
May cause vasoconstriction and cell proliferation7.9
Pulmonary artery
*Clinical significance in humans is unknown.
Prostanoid receptors in other systems throughout the body
There are 2 categories of prostanoid receptors in vascular cells1:
Vasodilative
Vasoconstrictive
Selexipag and its active metabolite are selective for the IP receptor vs other prostanoid receptors (EP1-4, DP, FP, and TP)6†
The clinical significance of this mechanism is unknown
Prostanoid receptors are located on various tissue types throughout the body1,8
Peripheral systemic artery
Gastrointestinal tract
Nerve cells
