A new intravenous (IV) formulation of selexipag (Uptravi®) has been approved by the US Food and Drug Administration (FDA) for the treatment of adults with World Health Organization (WHO) functional class II-III pulmonary arterial hypertension (PAH). The IV option will allow patients who are temporarily unable to take the oral tablet formulation of selexipag to continue treatment without interruptions.
“Given the progressive nature of this disease, maintaining treatment is important to help control PAH. However, there are times where patients may be unable to take oral medications,” said Kelly Chin, MD, Associate Professor of Internal Medicine and Director of the Pulmonary Hypertension Program at The University of Texas Southwestern Medical Center, Dallas. “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 retitrate Uptravi tablets after reinitiation,”
Dr. Chin was the senior author of the phase 3 clinical trial (NCT03187678) whose data the new approval was based on. The study recruited 20 patients with PAH to switch from their stable dose of selexipag tablets to a corresponding dose of IV selexipag and then back to tablets. The study involved an initial 28-day observation phase, a 12-day treatment and observation phase, and a 30-day safety follow-up.
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The treatment and observation phase was divided into 3 periods. During Period 1, patients received a morning and evening administration of their stable oral dose on Day 1. In Period 2, the patients received 3 corresponding IV doses of selexipag (an AM and PM dose on Day 2 and an AM dose on Day 3). Patients received an oral dose in the PM of Day 3 and then continued receiving twice-daily oral doses for 9 days.
Adverse events related to the IV administration of selexipag were consistent with those experienced during oral administration, except infusion site reactions experienced by 2 patients. The most common side effects of selexipag include headache, diarrhea, jaw pain, myalgia, extremity pain, flushing, and arthralgia.
Selexipag is a selective prostacyclin IP receptor agonist designed to delay the progression of PAH and decrease the risk of hospitalization in patients. It was discovered by Nippon Shinyaku and licensed to Actelion Pharmaceuticals, a Janssen Pharmaceutical Company of Johnson and Johnson. Initial FDA approval was granted for the oral formulation of selexipag in 2015.
References
Uptravi® (selexipag) receives FDA approval for intravenous use in adult patients with pulmonary arterial hypertension (PAH). News release. Janssen Pharmaceutical Companies of Johnson & Johnson; July 30, 2021.
Safety study of the switch from oral selexipag to intravenous Selexipag in subjects with stable pulmonary arterial hypertension. US National Library of Medicine. ClinicalTrials.gov. Accessed July 31, 2021.
Klose H, Chin KM, Ewert R, et al. Temporarily switching from oral to intravenous selexipag in patients with pulmonary arterial hypertension: safety, tolerability, and pharmacokinetic results from an open-label, phase III study. Respir Res. 2021;22(1):34. doi:10.1186/s12931-020-01594-8
