Last reviewed 2026-04-20 · How we verify

Uptravi (SELEXIPAG)

Uptravi works by activating the prostacyclin receptor, which helps to relax blood vessels and improve blood flow.

Uptravi (selexipag) is a small molecule prostacyclin receptor agonist developed by Actelion, targeting the prostacyclin receptor to treat pulmonary arterial hypertension and thromboembolic pulmonary hypertension. It was FDA approved in 2015 and is currently owned by Actelion. Uptravi is available as a branded medication, with two generic manufacturers. Key safety considerations include the risk of hypotension and fluid overload. As a prostacyclin receptor agonist, Uptravi works by mimicking the effects of prostacyclin, a naturally occurring substance that helps to relax blood vessels and improve blood flow.

At a glance

Mechanism of action

Selexipag is prostacyclin receptor (IP receptor) agonist that is structurally distinct from prostacyclin. Selexipag is hydrolyzed by carboxylesterase to yield its active metabolite, which is approximately 37-fold as potent as selexipag. Selexipag and the active metabolite are selective for the IP receptor versus other prostanoid receptors (EP1-4, DP, FP, and TP).

Approved indications

• Pulmonary arterial hypertension
• Thromboembolic pulmonary hypertension

Common side effects

• Headache
• Diarrhea
• Nausea
• Jaw pain
• Decreased appetite
• Pain in extremity
• Vomiting
• Flushing
• Arthralgia
• Rash
• Anemia
• Hyperthyroidism

Key clinical trials

• Individual Patient Expanded Access IND for Selexipag (Uptravi) in Participants With Non-healing Wound, Buerger's Disease
• A Clinical Study of to Confirm the Doses of Selexipag in Children With Pulmonary Arterial Hypertension (PHASE2)
• A Study of Selexipag as Add-On Treatment to Standard of Care in Children With Pulmonary Arterial Hypertension (PHASE3)
• A Study Providing Treatment Access in Participants With Pulmonary Hypertension Completing a Parent Study and Having no Other Option (PHASE3)
• Long-Term Outcomes of Selexipag in Schistosomiasis-Associated Pulmonary Arterial Hypertension
• Patient-Reported Outcomes and Adherence After Transition From Inhaled Iloprost to Oral Selexipag in Pulmonary Arterial Hypertension
• Selexipag (ACT-293987) in Pulmonary Arterial Hypertension (PHASE3)
• Study of ACT-293987 (NS-304) in Pulmonary Arterial Hypertension (PAH) (PHASE2)

Patents

Primary sources

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