Oops, looks like you need to register to access this feature.
Select “Keep Exploring” to look around Scholars in Medicine. You have full access to all videos and podcasts for a limited time. Registration is provided at no cost exclusively for healthcare providers.
Sign Up or Log In

Selexipag

Brand and Other Names: UPTRAVI
Mechanism of Action:

Selexipag is a prostacyclin receptor (IP receptor) agonist that is structurally distinct from prostacyclin. Selexipag is hydrolyzed by carboxylesterase 1 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 (EP ,DP, FP, and TP).

Indications:

UPTRAVI is a prostacyclin receptor agonist indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH.

Route: Oral
Dose:
  • UPTRAVI tablets starting dose: 200 mcg twice daily. 
  • Increase the dose by 200 mcg twice daily at weekly intervals to the highest tolerated dose up to 1600 mcg twice daily. 
  • Maintenance dose is determined by tolerability. 
  • Moderate hepatic impairment: Starting dose 200 mcg once daily, increase the dose by 200 mcg once daily at weekly intervals to the highest tolerated dose up to 1600 mcg. 
  • UPTRAVI for injection dose is determined by the patient's current dose of UPTRAVI tablets. Administer UPTRAVI for injection by intravenous infusion, twice daily. 
Adverse Reactions:

Adverse reactions occurring more frequently (≥5%) on UPTRAVI compared to placebo are headache, diarrhea, jaw pain, nausea, myalgia, vomiting, pain in extremity, and flushing. 

Contraindication:

Concomitant use with strong CYP2C8 inhibitors.
Hypersensitivity to the active substance or to any of the excipients. 

Warnings and Precautions:

Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment.

See package insert for full prescribing information.