Macitentan

Pulmonary arterial hypertension is a progressive, fatal rare cardiovascular disease. Patients experience a progressive increase in pulmonary vascular resistance, which eventually leads to right heart failure, with a 5-year survival rate of less than 50%. Macitentan is an anti-pulmonary arterial hypertension drug belonging to the class of endothelin receptor antagonists. By dual blocking of endothelin A and B receptors, it inhibits endothelin-induced pulmonary vasoconstriction, smooth muscle cell proliferation and fibrosis processes, effectively delaying disease progression. This drug is approved for the treatment of patients with pulmonary arterial hypertension of WHO functional class II to IV, which can reduce the risks of hospitalization and clinical deterioration in patients, and is currently one of the core therapeutic drugs for the long-term management of pulmonary arterial hypertension.

The global market size of macitentan was approximately USD 1.87 billion in 2023, and it is expected to grow at a compound annual growth rate of 4.2% to USD 2.3 billion by 2028. The growth momentum mainly comes from the improvement of the global diagnosis rate of pulmonary arterial hypertension and the improvement of patients' long-term medication compliance. In terms of the Chinese market, the terminal sales of macitentan in public medical institutions exceeded RMB 890 million in 2023. As this variety was included in the National Medical Insurance Catalogue in 2020, the accessibility of medication has been greatly improved. The market share of generic drugs has risen from 12% in 2021 to 47% in 2023, and the market competition between originator drugs and generic drugs tends to be balanced.

The original research enterprise of macitentan is Actelion, a subsidiary of Johnson & Johnson, and the original trade name is "Opsumit". The expiration date of its core compound patent in the United States is 2021, and the expiration date of the compound patent in China is 2022. The main dosage form approved for the original drug is tablet, with a specification of 10mg. It has been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and is also included in the FDA Reference Preparation Catalogue. Up to now, more than 12 Chinese enterprises have obtained the A status for their macitentan active pharmaceutical ingredients through CDE registration, and 8 domestic enterprises have obtained marketing approval for macitentan tablets, which are deemed to have passed the consistency evaluation. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO provides a full set of macitentan impurity reference standards, covering the full spectrum of impurities from synthesis process, degradation and metabolism. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards meet the quality requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can meet the full-process needs of API research and development, quality research and consistency evaluation.