Brimonidine

Glaucoma is the world's leading irreversible blinding eye disease, and high intraocular pressure is the core risk factor for its progression. Clinical practice has long been committed to exploring treatment regimens that combine hypotensive effects and optic nerve protection. Brimonidine is a highly selective α2 adrenergic receptor agonist. It can exert a hypotensive effect by reducing aqueous humor production, and increase aqueous humor outflow through the uveoscleral pathway. At the same time, it has a certain optic nerve protective effect. It is a first-line medication for patients with open-angle glaucoma and ocular hypertension, and can also be an important component of combined medication for angle-closure glaucoma. The applicable population covers glaucoma patients at all disease stages from early to middle and advanced stages, especially those intolerant to β-blockers.

At present, the global market size of anti-glaucoma drugs has exceeded 7 billion US dollars, among which the annual sales of brimonidine-related preparations have exceeded 1.2 billion US dollars, with a compound annual growth rate of 4.2% in the past three years. In the domestic market, the annual sales of brimonidine preparations are approximately 680 million yuan. With the increase in the popularity of glaucoma screening, the demand growth rate is stable at above 5.8%. In terms of the competitive landscape, the original research product still accounts for about 38% of the market share. Generic drugs from 11 domestic enterprises have been approved for marketing, and this variety has been included in the fifth batch of national centralized drug procurement. The winning bid price has decreased by an average of 72%, further promoting the improvement of clinical accessibility.

The original research enterprise of brimonidine is Allergan, and the original research trade name is Alphagan. The core compound patent of brimonidine expired in the United States in 2005, and the compound patent in China expired in 2008. At present, the dosage form of the original research product approved in China is ophthalmic preparation, with specifications including 0.1% (5ml:5mg) and 0.2% (5ml:10mg), which have been included in the *Catalogue of Reference Preparations for Chemical Drugs* issued by the National Medical Products Administration. As of now, there are 13 registration entries of brimonidine API on the China API Registration Platform, among which 8 are in status A (approved for use in marketed preparations). A total of 27 approval numbers are involved in the brimonidine preparations approved in China, covering eye drops, ophthalmic gels and other dosage forms. (Data as of October 2024, please refer to the official website of CDE for the latest information)

In response to the research and development and production quality control needs of brimonidine, CATO provides a full set of impurity reference standards for this API, covering all categories such as synthesis process impurities and degradation impurities. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All products meet the requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can fully meet the quality research needs of pharmaceutical enterprises in different scenarios such as registration and declaration, and daily release testing.