Bosentan

Pulmonary arterial hypertension is a rare cardiovascular disease with rapid progression and high fatality rate, and clinical treatment options have been very limited for a long time. Bosentan is the first oral endothelin receptor antagonist anti-pulmonary arterial hypertension drug. It competitively blocks the binding of endothelin to its receptors, reduces pulmonary vascular resistance, and effectively delays disease progression. Its indications cover idiopathic or hereditary pulmonary arterial hypertension in patients with WHO functional classification from grade Ⅱ to grade Ⅳ, and pulmonary arterial hypertension associated with connective tissue disease. It is also the first drug approved for the treatment of pulmonary arterial hypertension in children, filling the treatment gap for pediatric patients.

At present, the global market size of pulmonary arterial hypertension drugs has exceeded 8 billion US dollars, with an annual compound growth rate maintained at around 7%. Among them, endothelin receptor antagonists account for nearly 40% of the market. As a classic basic drug in this category, bosentan has a stable overall market demand. In terms of the domestic market, with the implementation of the medical insurance policy for rare diseases, the terminal sales of bosentan in public medical institutions exceeded 300 million yuan in 2023, and the market share of generic drugs has exceeded 75%. Up to now, more than 10 enterprises have obtained the approval documents for generic drugs, and the market competition has gradually become sufficient.

The original developer of bosentan is Actelion Pharmaceuticals, a subsidiary of Johnson & Johnson, and the original brand name is "Tracleer". Its core compound patent expired in 2015 in the United States, and the core patent in China expired in 2021. The main dosage forms approved for the original product include tablets, with specifications of 62.5mg and 125mg, as well as a 32mg dispersible tablet suitable for children. The original tablet has been included in the Catalogue of Marketed Drugs in China as a reference preparation, and is also listed in the FDA Reference Preparation Catalogue. In terms of domestic API registration, 12 enterprises including Huahai and Kelun have obtained CDE registration numbers for bosentan APIs, among which 9 are in Status A. The approved marketed preparation varieties cover both conventional tablets and dispersible tablets. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for bosentan API, which fully meet the requirements of pharmacopoeia regulations of multiple countries including the Chinese Pharmacopoeia and FDA. Most products are in regular stock, and orders placed before 16:00 can be shipped on the same day. It can fully meet the reference standard requirements of the whole process of drug research and development, quality research and production quality control, and help enterprises efficiently promote the R&D of relevant generic drugs and consistency evaluation work.