Selexipag

Selexipag is a first-in-class, orally available prostacyclin receptor agonist developed for the treatment of pulmonary arterial hypertension (PAH)—a progressive and life-threatening disease characterized by elevated pulmonary vascular resistance and right heart failure. As a non-prostanoid IP receptor agonist, Selexipag exerts its therapeutic effect through selective activation of the prostacyclin receptor, leading to vasodilation in the pulmonary vasculature, inhibition of platelet aggregation, and antiproliferative effects on vascular smooth muscle cells. Selexipag is supplied as a crystalline solid with a melting point of 134–138 °C. In pharmaceutical quality control contexts, Selexipag serves as a primary reference standard for analytical method development, method validation, and impurity profiling of selexipag-containing drug products. The compound's related substances—including Selexipag Impurity 1, Impurity 8, Impurity D, and N-Nitroso Selexipag Impurity 44—are officially recognized as critical quality attributes requiring strict control during commercial manufacturing. Selexipag represents a significant therapeutic advancement in PAH management, offering an oral alternative to parenteral prostacyclin therapies with a favorable pharmacokinetic profile and once- or twice-daily dosing. The structural complexity and therapeutic importance of Selexipag make it an essential API and reference material for pharmaceutical manufacturers and analytical laboratories worldwide.

 

 Product Parameters

---

Parameter	Specification
Product Name	Selexipag
CAS Number	475086-01-2
Molecular Formula	C₂₆H₃₂N₄O₄S
Molecular Weight	496.62 g/mol
Appearance	Yellow solid
Melting Point	134–138 °C
Density	1.210 ± 0.06 g/cm³ (predicted)
pKa	3.82 ± 0.40 (predicted)
Solubility	Slightly soluble in DMSO and methanol
Storage Condition	–20 °C Freezer

 

Application

---

Celsipag is an oral, highly selective, long-acting prodrug of the IP receptor agonist. It represents a potential therapeutic agent for various vascular diseases, such as pulmonary hypertension and obstructive arteriosclerosis.

 

Orphan drug for pulmonary hypertension

---

On December 21,2015, the U.S. FDA approved Selexipag (brand name Uptravi), a novel drug developed by Actelion, for use in the treatment of adult patients with pulmonary hypertension. Selexipag is an oral ipprostacyclin receptor agonist that relaxes vascular wall smooth muscle, dilates blood vessels, and reduces pulmonary artery pressure. It has been designated as an orphan drug by the U.S. FDA. Pulmonary hypertension is a chronic, progressive pulmonary disorder with a poor prognosis, where patients may experience premature death or require lung transplantation.

 

Product Advantages

---

        Clinically Validated Prostacyclin Receptor Agonist

Selexipag is a first-in-class, orally available non-prostanoid agonist of the prostacyclin (IP) receptor, indicated for the treatment of pulmonary arterial hypertension (PAH). It demonstrates high selectivity for the human IP receptor (Ki = 260 nM) with minimal affinity for other prostanoid receptors (EP1-4, DP, FP, and TP: >10 μM).

 

Prodrug Design for Enhanced Oral Bioavailability

Selexipag functions as a prodrug that is readily hydrolyzed in vivo to the active metabolite ACT-333679 (MRE-269), which is itself a potent and selective agonist at IP receptors. This prodrug strategy enables oral administration with favorable pharmacokinetics and once- or twice-daily dosing, offering a significant advantage over parenteral prostacyclin therapies.

 

Distinctive Pyrazine-Based Structure

Selexipag features a unique pyrazine core with two phenyl groups at positions 5 and 6, an isopropylamino substituent linked via a butoxy chain to an N-(methylsulfonyl)acetamide moiety. This distinctive structure classifies Selexipag as a monocarboxylic acid amide, ether, aromatic amine, tertiary amine, and N-sulfonylcarboxamide.

 

Dual-Use: API and Reference Standard

Cosperpharm supplies Selexipag at multiple quality levels: research grade (≥98% HPLC) for process development applications; and reference standard grade (≥95% HPLC with full characterization) for use in analytical method development, method validation, QC testing, and ANDA filing. The compound is also used to monitor related substances including Selexipag Impurity 1, Impurity 8, Impurity D, and N-Nitroso Selexipag Impurity 44.

 

Broad Research and Analytical Utility

Selexipag serves as a critical reference standard for pharmaceutical quality control, enabling analytical method development, system suitability testing, specificity studies, and impurity profiling as part of ICH Q2(R1)-compliant validation. Its unique structural features make it a valuable compound for medicinal chemistry research and drug discovery programs targeting the prostacyclin pathway.

 

Contact Us

---

Securing Selexipag for your PAH drug manufacturing campaign, impurity profiling program, or analytical method development should be straightforward. Cosperpharm makes it simple with high-quality reference standards, comprehensive documentation, and responsive technical support. Contact us today to discuss your requirements—we're here to help you succeed.