Selexipag

Pulmonary arterial hypertension is a rare cardiopulmonary vascular disease with rapid progression and high fatality rate. For a long time, there has been a lack of oral treatment regimens with both tolerability and long-term benefits in clinical practice. As the first oral selective prostacyclin IP receptor agonist, selexipag can dilate pulmonary vascular smooth muscle, inhibit vascular remodeling and platelet aggregation through long-acting activation of IP receptors. It not only overcomes the limitations of traditional prostacyclin drugs such as the need for intravenous administration and short half-life, but also reduces the risk of adverse reactions caused by non-selective receptor activation. At present, the drug is mainly used to treat adult patients with pulmonary arterial hypertension of World Health Organization functional class Ⅱ-Ⅲ. It can significantly reduce the risk of disease deterioration, and long-term use can effectively improve the exercise tolerance and quality of life of patients.

At this stage, the global market size of pulmonary arterial hypertension treatment has exceeded 8 billion US dollars, of which targeted drugs account for more than 90%. As the core oral variety of prostacyclins, selexipag has a peak annual sales of nearly 1.2 billion US dollars. The base of pulmonary arterial hypertension patients in China is about 3 million to 5 million. With the implementation of the medical insurance policy for rare diseases, after selexipag was included in the national medical insurance catalog in 2021, the annual growth rate of the domestic market has remained above 35% for a long time. At present, the domestic preparation market is still dominated by the original research drug, and a number of enterprises have laid out the research and development of generic drugs. With the expiration of core patents, the launch of generic drugs will further improve the accessibility of drugs and drive the rapid expansion of upstream API demand.

The original research enterprise of selexipag is Actelion Pharmaceuticals Ltd. of Switzerland (a subsidiary of Johnson & Johnson), and the original trade name is Uptravi®. The expiration time of its core compound patent in China is 2029, and the expiration time of the crystal form patent is 2031. The main dosage form approved by the original research is tablet, with 8 titration specifications including 0.2mg, 0.4mg, 0.6mg, 0.8mg, 1.0mg, 1.2mg, 1.4mg and 1.6mg. It has been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and also included in the reference preparation catalogue of FDA. Up to now, there is no domestic selexipag preparation approved in China, and no A-status registration number submitted by any enterprise on the API registration platform. Only the original preparation product has been approved for import and marketing. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for selexipag API, which fully meets the needs of the whole process of synthetic process research and development, quality research, and generic drug declaration. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All impurities comply with the compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and complete structure confirmation and calibration reports can be provided with the goods to help customers accelerate the research and development and declaration process.