Betaxolol

There are more than 76 million patients with glaucoma worldwide. As an irreversible blinding eye disease, long-term intraocular pressure reduction is the core intervention to delay the progression of the disease. Betaxolol is a selective β1 adrenergic receptor blocker. It reduces aqueous humor production by blocking β1 receptors on non-pigmented ciliary epithelial cells, and can lower intraocular pressure by 20% to 30%. It has almost no pulmonary adverse reactions related to β2 receptors, so it is especially suitable for glaucoma patients with asthma and chronic obstructive pulmonary disease, and can also be used as a second-line treatment for hypertension, providing a safer option for clinical needs in the intersecting field of cardiology and ophthalmology.

According to public data, the global market size of anti-glaucoma drugs was approximately USD 6.8 billion in 2023, of which β-blockers accounted for about 12%. Benefiting from its cardiovascular safety advantage, betaxolol has a compound annual growth rate of 4.7% in the recent 3 years, which is higher than the average level of similar products. In the Chinese market, the original research product still accounts for about 42% of the market share, and 6 domestic enterprises have obtained the approval documents for generic drug preparations. Since betaxolol was included in the National Medical Insurance Catalog in 2021, the domestic drug use scale has continued to rise, and the in-hospital sales increased by 18.2% year-on-year in 2023, and the demand for domestic substitution of APIs is gradually released.

The original research enterprise of betaxolol is Janssen Pharmaceuticals, a subsidiary of Johnson & Johnson, and the original brand name is "Betoptic". Its core compound patent expired in the United States in 2006, and the compound patent in China expired in 2005. The main dosage forms approved for the original product are eye drops, with specifications of 0.25% (5ml:12.5mg) and 0.5% (5ml:25mg). It has been included in the Catalogue of Listed Drugs in China as the reference listed drug, and is also included in the FDA Reference Listed Drug Catalog. Up to now, there are 4 registration entries of betaxolol APIs on the API Registration Platform of China CDE, among which 2 are in Status A. There are 7 betaxolol preparation products approved for marketing in China, covering two dosage forms: eye drops and tablets. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for betaxolol API, covering all impurity types related to the synthesis process and degradation pathways. Most products are available in stock. Orders placed before 16:00 can be shipped on the same day. All reference standards meet the requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA, and can fully meet the reference substance needs of the whole process of API R&D, quality research and registration declaration.