The Prostacyclin Pathway Is 1 of 3 Foundational Pathways That Are Targets for Drug Therapy1,2
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
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
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Median time from PAH diagnosis in patients taking UPTRAVI®: 0.9 years
This article includes information that has not been approved by the Food and Drug Administration for UPTRAVI® (selexipag). Please see full Prescribing Information available on this website. Authors[s] of this article have received remuneration from Actelion Pharmaceuticals US, Inc., or its affiliates.
*Other=drugs and toxins (2%) and HIV (1%).
6MWD=6-minute walk distance; ERA=endothelin receptor antagonist; FC=Functional Class; GRIPHON=Prostacyclin (PGI2) Receptor Agonist In Pulmonary Arterial HypertensiON; HIV=human immunodeficiency virus; HPAH=heritable PAH; IPAH=idiopathic PAH; PAH-CHD=PAH associated with congenital heart disease with repaired shunts; PAH-CTD=PAH associated with connective tissue disease; PDE5i=phosphodiesterase type-5 inhibitor; WHO=World Health Organization.
1. UPTRAVI® (selexipag) full Prescribing Information. Actelion Pharmaceuticals US, Inc. 2. Sitbon O, Gomberg-Maitland M, Granton J, et al. Clinical trial design and new therapies for pulmonary arterial hypertension. Eur Respir J. 2019;53(1):1801908. doi:10.1183/13993003.01908-2018 3. Data on file. Actelion Pharmaceuticals US, Inc. Length and Population Size of PAH Pivotal Trials Confirmation. June 2024. 4. Sitbon O, Channick R, Chin KM, et al. Selexipag for the treatment of pulmonary hypertension. N Engl J Med. 2015;373:2522-2533 and suppl. 5. Data on file. Actelion Pharmaceuticals US, Inc. GRIPHON Baseline Characteristics Study Report.