BETHESDA, MD 23 Dec 2015—FDA and Actelion Pharmaceuticals US Inc. on Tuesday announced the approval of selexipag, or Uptravi, for the treatment of pulmonary arterial hypertension.
When taken long term, selexipag can reduce hospitalization for pulmonary arterial hypertension and the risk of disease progression compared to placebo, FDA said.
The labeling for selexipag (PDF), a prostacyclin-receptor agonist, recommends a starting dosage of 200 µg twice daily. This dosage is to be increased, usually at weekly intervals, by increments of 200 µg twice daily up to the maximum a patient can endure or 1600 µg twice daily, whichever is less.
In patients with moderate hepatic impairment, the dosing interval should be once daily. This recommendation in the labeling is based on pharmacokinetic modeling of data from people with hepatic impairment. The Phase III study of selexipag in patients with pulmonary arterial hypertension excluded anyone with moderate or severe hepatic impairment, according to ClinicalTrials.gov. The labeling for selexipag recommends avoiding therapy with the drug in patients with severe hepatic impairment.
Taking selexipag doses with food, the labeling states, may improve a patient's tolerability of the therapy. According to the Pharmacokinetics section of the labeling, food delays the time to peak plasma concentration of selexipag and lowers its peak plasma concentration yet does not significantly change overall exposure to the drug and its active metabolite.
Headache was reported in 65% of the patients who received selexipag during the Phase III study, according to the labeling. Diarrhea occurred in 42%. Nausea occurred in 33%. These and other adverse reactions occurred more frequently during the weeks of dosage adjustment than when patients were taking their maximum dosage.
Uptravi will be supplied in eight tablet strengths ranging from 200 µg to 1600 µg.
All strengths of Uptravi will be available in 60-count bottles. Only the 200-µg tablets will be available in a 140-count bottle.
The tablets are film coated and are not to be split, crushed, or chewed.
Actelion stated that the company expects its new product to be available to U.S. patients in early 2016.