Theophylline

Chronic respiratory diseases are one of the types of chronic diseases with high incidence worldwide. The patient population of bronchial asthma, chronic obstructive pulmonary disease (COPD) and other diseases is large, and there is a long-term clinical demand for safe and economical anti-asthmatic drugs. As a classic methylxanthine anti-asthmatic drug, theophylline exerts multiple effects of relaxing bronchial smooth muscle, anti-inflammation and enhancing diaphragmatic contractility by inhibiting phosphodiesterase, increasing the level of intracellular cyclic adenosine monophosphate, antagonizing adenosine receptors and reducing intracellular calcium ion concentration. It can be used for symptom control after acute asthma attack, and also as a long-term maintenance treatment for COPD in stable stage, covering the treatment needs of adult and pediatric patients with respiratory diseases.

At present, the global market size of theophylline drugs is about USD 1.8 billion, with a compound annual growth rate maintained at around 2.3%. The growth momentum mainly comes from the improvement of the diagnosis and treatment rate of respiratory diseases in low- and middle-income countries. The market size of domestic theophylline preparations is about RMB 1.2 billion. As the compound patent has long expired, the market is dominated by generic drugs, with more than 60 manufacturers. Among them, ordinary tablets, sustained-release tablets, injections and other dosage forms have been included in multiple batches of national centralized procurement, and the winning bid price has decreased by more than 70% on average compared with before, which further expands the accessibility of grass-roots medication and also drives the steady increase in the demand for upstream APIs.

The original research enterprise of theophylline is Germany's Boehringer Ingelheim, with the original trade name Theograd. The core compound patent expired in major global markets in the 1970s. At present, the mainstream dosage forms include sustained-release tablets (100mg, 200mg, 300mg) and injections (10ml:0.25g). Its sustained-release tablets have been included in the *Catalogue of Reference Preparations for Chemical Drugs* of China and also listed in the FDA Reference Preparation Catalogue. According to the domestic API registration platform, 23 enterprises have obtained A-status registration numbers for theophylline APIs, which can meet the supporting needs of domestic preparation production. The domestically approved and marketed theophylline preparations cover multiple dosage forms such as ordinary tablets, sustained-release capsules, injections and suppositories. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of impurity reference standards for theophylline API, with most products in stock. In-stock products ordered before 16:00 will be shipped on the same day. They meet the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can fully support the quality control needs of pharmaceutical enterprises in R&D and production links such as API quality research and preparation consistency evaluation, effectively reducing the time cost of the supply chain in the R&D stage.