Upadacitinib

In response to the unmet clinical needs for autoimmune diseases such as moderate-to-severe atopic dermatitis and rheumatoid arthritis, the advent of highly selective JAK inhibitors provides patients with a new option for targeted therapy. As a JAK1 subtype selective inhibitor, upadacitinib can block the JAK-STAT signaling pathway and inhibit the release of a variety of pro-inflammatory cytokines, thereby reducing inflammatory responses and slowing down disease progression. At present, its globally approved indications cover rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, ankylosing spondylitis, and non-radiographic axial spondyloarthritis. It is mainly used for moderate-to-severe patients aged 12 and above who have insufficient response, loss of response, or intolerance to conventional therapy or biological agents. Clinical evidence has confirmed that it has better safety characteristics than some non-selective JAK inhibitors.

The global market size of upadacitinib has exceeded US$9.2 billion in 2023, with a compound annual growth rate of over 110% from 2019 to 2023, making it one of the fastest-growing therapeutic drugs for autoimmune diseases at present. In terms of the domestic market, upadacitinib has achieved rapid volume growth after being included in the national medical insurance catalog in 2022, and its terminal sales in public medical institutions exceeded RMB 1.6 billion in 2023. Currently, 3 generic drugs of upadacitinib have been approved for marketing in China, while the original drug still accounts for about 70% of the market share. On the API supply side, it is still dominated by in-house production of the original manufacturer and imported cooperation, and there is no public data on the large-scale domestic production and marketing of upadacitinib API.

The original research enterprise of upadacitinib is AbbVie, and the original brand name is Rinvoq. Its core compound patent will expire in 2029 in the United States and in 2028 in China. The original dosage form approved in China is sustained-release tablets, with specifications of 15mg and 30mg. The original sustained-release tablets have been included in the *Catalogue of Reference Preparations for Chemical Drugs (49th Batch)* issued by the National Medical Products Administration. Up to now, the CDE API Registration Platform has not yet announced the approved registration number of upadacitinib API. The upadacitinib preparations approved in China include the original product and 3 domestic generic drugs. (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 upadacitinib API. The products are developed and produced in strict compliance with the requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA. Most of the impurity reference standards are regularly in stock. In-stock orders placed before 16:00 can be shipped on the same day, which can provide stable reference standard support for pharmaceutical enterprises in API synthesis process optimization, quality research and preparation registration.