Tofacitinib

Autoimmune diseases such as rheumatoid arthritis and psoriasis have long relied on hormones and traditional disease-modifying antirheumatic drugs, with insufficient response rates and high risks of adverse reactions. The advent of JAK pathway inhibitors has brought new targeted therapy options for such patients. Tofacitinib is a JAK1/JAK3 inhibitor, which selectively inhibits the activity of the JAK kinase family and blocks the signal transduction of various pro-inflammatory cytokines such as IL-6 and IFN-γ. It is clinically used for the treatment of moderate to severe active rheumatoid arthritis, active psoriatic arthritis, ulcerative colitis and other diseases. It can be used as a single agent or in combination with non-biological disease-modifying antirheumatic drugs such as methotrexate, and is suitable for adult patients with insufficient response or intolerance to traditional treatments.

The global market size of tofacitinib exceeded US$9 billion in 2022, and the compound annual growth rate from 2023 to 2029 is expected to remain at around 3.2%. In terms of the Chinese market, with the improvement of the diagnosis rate of autoimmune diseases and the expansion of medical insurance coverage, the sales of tofacitinib in public medical institutions exceeded RMB 1.2 billion in 2023, and the market share of generic drugs has exceeded 75%. At present, nearly 30 domestic enterprises have obtained the approval documents for tofacitinib preparations. In addition to imported original research suppliers on the API supply side, 18 domestic enterprises have completed API registration, the overall competitive landscape is relatively sufficient, and the downward cost has further improved the accessibility of drugs for patients.

The original research enterprise of tofacitinib is Pfizer, with the trade name Xeljanz. Its core compound patent will expire in the United States in 2025, and the Chinese compound patent expired in 2020. The main dosage forms of the original research product include tablets and sustained-release tablets. The specification of the tablets is 5mg, and the specifications of the sustained-release tablets are 11mg and 22mg. Relevant dosage forms have been included in the Catalogue of Marketed Drugs in China as reference preparations, and are also included in the FDA Reference Preparation Catalogue. Up to now, 18 domestic enterprises in China have obtained A status for their tofacitinib APIs through CDE registration, and the approved and marketed preparations include conventional tablets and sustained-release tablets, covering all marketed specifications. (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 tofacitinib API. Most products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day, which can meet the multi-scenario needs in the R&D and registration stages. All products comply with the compliance requirements of multiple regulations such as Chinese Pharmacopoeia and FDA, and can effectively help enterprises shorten the R&D cycle and reduce registration risks.