The Prostacyclin Pathway Is 1 of 3 Proven Signaling Pathways That Are Targets for Drug Therapy1
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 artery2,4
Three established prostanoid receptors in the human pulmonary artery4
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)2†
The clinical significance of this mechanism is unknown
†DP1, EP2, EP4, EP1, and FP are not functionally expressed in the pulmonary artery and do not contribute to vessel tone in the pulmonary artery.
GRIPHON=Prostacyclin (PGI2) Receptor Agonist In Pulmonary Arterial HypertensiON.
References:1. Lang MI, Gaine SP. Recent advances in targeting the prostacyclin pathway pulmonary arterial hypertension. Eur Respir Rev. 2015;24(138):630-641. 2. UPTRAVI® (selexipag) full Prescribing Information. Actelion Pharmaceuticals US, Inc. 3. Gale S. The evolving treatment landscape of pulmonary arterial hypertension. Am J Manag Care. 2012;27(3 Suppl):S42-S52. doi:10.37765/ajmc.2021.88610 4. Norel X. Prostanoid receptors in the human vascular wall. ScientificWorldJournal. 2007;7:1359-1374. 5. Mubarak KK. A review of prostaglandin analogs in the management of patients with pulmonary arterial hypertension. Respir Med. 2010;104(1):9-21. 6. Capra V, Bäck M, Angiolillo DJ, et al. Impact of vascular thromboxane prostanoid receptor activation on hemostasis, thrombosis, oxidative stress, and inflammation. J Thromb Haemost. 2014;12(2):126-137.
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After the starting dose of 200 mcg twice daily, all patients completed titration to their maintenance dose within the first 12 weeks, up to a maximum dose of 1600 mcg twice daily.
Primary endpoint: time to first PAH disease progression event
Death
Hospitalization for PAH
Need for lung transplantation or balloon atrial septostomy for worsening of PAH
Parenteral prostanoid or chronic oxygen therapy
Other disease progression (decrease in 6MWD plus worsening of FC or need for other therapy)
Baseline patient characteristics
Mean age: 48 years
Female: 80%
*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; PDE-5i=phosphodiesterase type-5 inhibitor; WHO=World Health Organization.
References: 1. UPTRAVI® (selexipag) full Prescribing Information. Actelion Pharmaceuticals US, Inc. 2. Ruopp NF, Cockrill BA. Diagnosis and treatment of pulmonary arterial hypertension: a review. JAMA. 2022;327(14):1379-1391. 3. Sitbon O, Channick R, Chin KM, et al. Selexipag for the treatment of pulmonary arterial hypertension. N Engl J Med. 2015;373:2522-2533. 4. Coghlan JG, Channick R, Chin K, et al. Targeting the prostacyclin pathway with selexipag in patients with pulmonary arterial hypertension receiving double combination therapy: insights from the randomized controlled GRIPHON study. Am J Cardiovasc Drugs. 2018;18(1):37-47.
UPTRAVI® WAS STUDIED IN GRIPHON, A LARGE OUTCOMES TRIAL IN PAH (N=1156)1
After the starting dose of 200 mcg twice daily, all patients completed titration to their maintenance dose within the first 12 weeks, up to a maximum dose of 1600 mcg twice daily.
Primary endpoint: time to first PAH disease progression event
Death
Hospitalization for PAH
Need for lung transplantation or balloon atrial septostomy for worsening of PAH
Parenteral prostanoid or chronic oxygen therapy
Other disease progression (decrease in 6MWD plus worsening of FC or need for other therapy)
Baseline patient characteristics
Mean age: 48 years
Female: 80%
*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; PDE-5i=phosphodiesterase type-5 inhibitor; WHO=World Health Organization.
Reference: 1. UPTRAVI® (selexipag) full Prescribing Information. Actelion Pharmaceuticals US, Inc.
