Proxyphylline

Among respiratory diseases, airway spasm symptoms caused by bronchial asthma and chronic obstructive pulmonary disease (COPD) often lead to impaired ventilatory function in patients, which seriously affects their quality of life. Proxyphylline, as a xanthine anti-asthmatic drug, inhibits phosphodiesterase activity to increase the concentration of cyclic adenosine monophosphate in cells, and antagonizes adenosine receptors at the same time, exerting multiple effects including relaxing bronchial smooth muscle, strengthening cardiac function, inducing diuresis and dilating coronary arteries. Clinically, it is mainly used to relieve wheezing symptoms caused by asthma, asthmatic bronchitis and COPD, and can also be used for asthma caused by cardiogenic pulmonary edema, especially suitable for adult and elderly patients with good tolerance to theophylline drugs. Compared with aminophylline, it has milder gastrointestinal adverse reactions and higher clinical compliance.

In the global anti-asthmatic drug market, xanthines, as basic medications, have long occupied a stable market share. Among them, proxyphylline has a global market size of approximately USD 320 million in 2023 due to its safety advantages, with a compound annual growth rate maintained at 2.8%. In terms of the domestic market, the demand for cost-effective anti-asthmatic drugs in primary medical institutions continues to be released. The annual sales of proxyphylline preparations exceed RMB 700 million. At present, more than 30 enterprises have obtained the approval documents for generic preparations. After the centralized procurement, the price of preparations has dropped by 62%, and the demand for upstream API has risen simultaneously. Domestic API manufacturers are mainly pharmaceutical enterprises in East China and South China, and leading enterprises account for about 45% of the market share.

The original research enterprise of proxyphylline is Mitsubishi Tanabe Pharma, and the original research brand name is Neophyllin. Its core compound patent expired worldwide in 1985. The main dosage forms of the original research marketed products include tablets (200mg) and injections (2mL:0.2g), which have been included in the reference preparation catalog of the Pharmaceuticals and Medical Devices Agency (PMDA) of Japan, and the original research preparations have not been imported into China. At present, there are 12 domestic registration numbers for proxyphylline API, 8 of which are in A status and can be supplied for the production of generic preparations. The domestically approved preparation varieties cover three categories: tablets, injections and proxyphylline for injection. (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 proxyphylline API. Most of the products are available in stock. Spot orders paid before 16:00 can be shipped on the same day. All reference standards comply with the regulatory requirements of drug regulatory authorities of various countries such as the Chinese Pharmacopoeia and FDA, with complete data on impurity structure confirmation and purity detection, which can directly support the R&D needs at different stages such as API quality research and generic drug consistency evaluation.