Products
Selexipag was approved in the United States in 2015 and in the EU and many countries in 2016 in film-coated tablet form (Uptravi).
Structure and properties
Selexipag (C26H32N4O4S, Mr = 496.6 g/mol) is a diphenylpyrazine derivative. It is biotransformed in the liver by carboxylesterase 1 (CES1) to the active metabolite ACT-333679 (MRE-269). The metabolite has a higher binding affinity and is involved in the effect. Selexipag is structurally distinct from prostacyclin and other prostacylin receptor agonists. It exists as a pale yellow crystalline powder that is virtually insoluble in water. The substance is stable, non-hygroscopic and non-photosensitive.
Effects
Selexipag (ATC B01AC27) has vasodilatory, antifibrotic, and antiproliferative properties. The effects are due to selective agonism at the IP receptor (prostacyclin receptor) on vascular smooth muscle. In pulmonary arterial hypertension, IP receptor expression and prostacyclin synthesis are reduced, contributing to disease development. Selexipag is characterized by its selectivity and oral availability. It does not bind to other prostanoid receptors.
Indications
For the treatment of pulmonary arterial hypertension (PAH) in patients with advanced functional limitation (NYHA functional classes III/IV) to delay disease progression.
Dosage
According to the SmPC. Tablets are taken in the morning and evening with a meal.
Contraindications
- Hypersensitivity
Full details of precautions and interactions can be found in the drug label.
Adverse effects
Possible adverse effects include headache, diarrhea, nausea, vomiting, jaw pain, muscle pain, pain in the extremities, flushing, and joint pain.
