Upadacitinib Pharmacology

Upadacitinib (Upadacitinib) is a selective Janus kinase (JAK) inhibitor that can effectively inhibit JAK1, but has a weak inhibitory effect on other JAK subtypes. The JAK/STAT (signal transducer and activator of transcription) pathway is involved in regulating not only innate and adaptive immune mechanisms, but also inflammatory responses. Therefore, this pathway has become a target for the development of treatments for immune diseases.

The JAK enzyme family consists of 4 members: JAK1 and tyrosine kinase 2 (tyk 2). Inhibition of JAK1 signaling inhibits interleukin-6 pro-inflammatory signaling, which is thought to be a major factor in clinical efficacy in immune diseases. In contrast, the JAK2 downstream signaling cascade regulates the expression of interleukin-3, interleukin-5, erythropoietin, and thrombopoietin, which contribute to erythropoiesis and myelopoietin. Upadatinib has enhanced selectivity for JAK1 and has the potential to offer robust efficacy and an acceptable safety profile in multiple Phase 2 and 3 studies in patients with rheumatoid arthritis (RA), as well as in Phase 2 studies in patients with Crohn's disease and atopic dermatitis. Upadatinib is also accepted to treat psoriatic arthritis, ulcerative colitis, and ankylosing spondylitis.

The original drug Upatinib has been launched in China, and has subsequently entered the scope of Class B medical insurance. Only eligible patients can be reimbursed. Specifications The price of each box of 15mg*28 tablets may be around RMB 3,000. The European version of the original drug sold overseas is priced at more than 20,000 yuan for 15mg*30 tablets (the price may fluctuate due to exchange rates), which is expensive. Cheaper upadatinib generic drugs are also sold overseas, and their pharmaceutical ingredients are basically the same as those of the original drugs sold domestically and abroad. For example, the price of 15mg*30 tablets produced by Bangladesh pharmaceutical factory is around 900 yuan (the price may fluctuate due to the exchange rate).