Aprocitentan

Pulmonary arterial hypertension is a progressive, highly fatal rare cardiovascular disease. The persistent elevation of pulmonary vascular resistance in patients can eventually lead to right heart failure, and there has been a long-term clinical lack of highly specific targeted treatment regimens. Macitentan is an anti-pulmonary arterial hypertension drug belonging to the endothelin receptor antagonist class. It blocks the pathological processes such as endothelin-mediated vasoconstriction and smooth muscle proliferation by dual blocking of ETA and ETB receptors. Compared with the first-generation single-target endothelin receptor antagonists, its risk of hepatotoxicity is significantly reduced, and the safety of long-term medication is better. At present, this drug is approved for the treatment of patients with pulmonary arterial hypertension of WHO functional class II to IV. It can effectively delay disease progression and reduce the risk of hospitalization, and is a first-line long-term treatment drug recommended by domestic and foreign guidelines.

At present, the global market size of targeted drugs for pulmonary arterial hypertension has exceeded 8 billion US dollars, among which endothelin receptor antagonists account for more than 35%. With a lower incidence of adverse reactions, macitentan has maintained a compound annual growth rate of around 12% in the past three years. In terms of the domestic market, with the coverage of medical insurance policies for rare diseases, the hospital sales of macitentan exceeded 320 million yuan in 2023, an increase of 47% over the previous year. At present, the original research product still occupies more than 90% of the market share, and 5 domestic pharmaceutical companies have submitted marketing applications for generic drugs. With the expiration of core patents, the generic drug substitution space is expected to exceed 2 billion yuan.

The original research enterprise of macitentan is Actelion Pharmaceuticals in the United States, and the original research trade name is "Opsumit". The expiration date of its core compound patent in China is October 2026. The dosage form of the original research product approved in China is oral tablet, with a specification of 10 mg. It has been included in the *Reference Preparations Catalogue of Chemical Drugs* issued by the National Medical Products Administration, and is also listed in the FDA Reference Preparations Catalogue. Up to now, the China NMPA has approved the marketing of the original research macitentan tablets. There is no approved domestic macitentan registration number on the CDE API registration platform, and only the API registration applications submitted by 3 enterprises are in the review and approval stage. (Data as of June 2025, please refer to the official CDE website for the latest information)

In response to the core demands such as impurity research and quality control in the development process of macitentan generic drugs, CATO provides a full set of impurity reference standards for this API. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. The products fully comply with the regulatory requirements of the Chinese Pharmacopoeia, FDA and other regulations, which can effectively shorten the R&D cycle and reduce compliance risks.