The Food and Drug Administration (FDA) has approved Uptravi® (selexipag) injection for intravenous (IV) use for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH in adults with WHO Functional Class II-III, who are temporarily unable to take oral therapy.
The approval was based on data from a prospective, multicenter, open-label, single sequence cross-over phase 3 study (ClinicalTrials.gov Identifier: NCT03187678) that evaluated the safety, tolerability and pharmacokinetics of temporarily switching between the tablet and IV formulation of selexipag in 20 PAH patients who were previously receiving a stable oral dose of the drug. The study investigated switching from Uptravi tablets to a corresponding IV infusion and then back to tablets.
Findings showed that the switch between the tablet and IV formulation was well tolerated with no unexpected safety findings and comparable exposure to the active metabolite. A comparison of the safety profiles for the 2 formulations showed similarity, with the exception of infusion site reactions for the IV formulation. The most common adverse reactions were headache, diarrhea, jaw pain, nausea, myalgia, vomiting, pain in extremity, and flushing.
“For patients on Uptravi, bridging short-term temporary interruptions of Uptravi tablets with Uptravi IV may maintain the treatment effect and avoid the need to change therapy or re-titrate Uptravi tablets after re-initiation,” said Kelly Chin, MD, Uptravi IV study senior author and Associate Professor of Internal Medicine and Director of the Pulmonary Hypertension Program at The University of Texas Southwestern Medical Center.
Uptravi for injection is supplied as a 10mL single-dose vial containing 1800mcg of selexipag. The IV dose is determined by the patient’s current dose of tablets.
- Uptravi® (selexipag) receives FDA approval for intravenous use in adult patients with pulmonary arterial hypertension (PAH). News release. Janssen Pharmaceutical Companies. Accessed July 30, 2021. https://www.prnewswire.com/news-releases/uptravi-selexipag-receives-fda-approval-for-intravenous-use-in-adult-patients-with-pulmonary-arterial-hypertension-pah-301345104.html.
- Uptravi [package insert]. South San Francisco, CA: Actelion Pharmaceuticals US; 2021.