Timolol

β-blockers are a classic therapeutic category in the fields of cardiovascular disease and ophthalmology. Among them, timolol, a non-selective β-blocker, has been in clinical application for more than 40 years due to its unique action advantages. This drug blocks β-adrenergic receptors to reduce aqueous humor production and thus lower intraocular pressure. Meanwhile, it can inhibit sympathetic nerve excitation, slow down heart rate and reduce myocardial oxygen consumption. Clinically, it is mainly used for long-term intraocular pressure control in primary open-angle glaucoma, and can also be used for hypertension, prognosis improvement of myocardial infarction and migraine prevention. Its applicable population covers adult patients with chronic diseases and some adolescent patients who need intraocular pressure control, and it is a first-line basic drug recommended by multiple clinical guidelines.

The global market size of timolol is stable at around USD 620 million, among which ophthalmic dosage forms account for more than 75%, with a compound annual growth rate of 2.8% in the past five years. The growth momentum mainly comes from the continuous increase in the prevalence of glaucoma and the release of demand for primary care medication for chronic cardiovascular diseases. In terms of the domestic market, timolol preparations have been included in the National Essential Medicines List. In 2023, the terminal sales in public medical institutions were approximately RMB 210 million, among which eye drops accounted for more than 90%. The competitive landscape is dominated by generic enterprises. At present, more than 20 enterprises have obtained production approvals for eye drops, the supply of active pharmaceutical ingredients has been localized, the overall price is at a relatively low level, and the accessibility is high.

The original research enterprise of timolol is Merck Sharp & Dohme, with the original brand name Timoptic. The core compound patent expired in the United States in 1985, and the compound patent in China has expired. The main dosage forms approved by the original research include eye drops (0.25% and 0.5% specifications) and tablets (5mg and 10mg specifications). Its 0.5% eye drops have been included in the FDA Reference Listed Drug Catalog, and also included in the *Catalogue of Reference Preparations for Chemical Drugs (20th Batch)* of China. In terms of domestic API registration, 8 enterprises have completed the registration of timolol API in CDE (status A) so far, and more than 30 domestic enterprises have obtained marketing approval for timolol eye drops and tablets. (Data as of October 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of impurity reference standards for timolol API. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. They fully meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can fully meet the needs of API manufacturers in quality research, stability study and registration declaration.