SYK inhibitor R406 (CAS: 841290-80-0) is a small-molecule inhibitor of the spleen tyrosine kinase (SYK) developed by Rigel Pharmaceuticals for the treatment of various autoimmune and inflammatory diseases, such as rheumatoid arthritis, lupus, and asthma. SYK is a key mediator of signaling pathways involved in immune cell activation, cytokine production, and inflammation.
Chemical name: (5Z)-5-[(5-fluoro-2-methylphenyl)methylene]-2-[4-(morpholin-4-yl)phenyl]-2,4-dihydro-3H-pyrazol-3-one
Molecular formula: C20H21FN4O2
Formula weight: 362.41 g/mol
CAS No: 841290-80-0
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Health benefits of this product: SYK inhibitor R406 has shown potential in preclinical and clinical studies for the treatment of various autoimmune and inflammatory diseases, such as rheumatoid arthritis, lupus, and asthma. It works by inhibiting the activity of the SYK kinase, which plays a crucial role in the activation of immune cells, such as B cells, mast cells, and macrophages. By blocking SYK, R406 can potentially reduce inflammation, autoantibody production, and tissue damage in these diseases.
Potential effects: R406 has shown promising results in preclinical and clinical studies for the treatment of rheumatoid arthritis, lupus, and asthma. In particular, it has demonstrated efficacy in reducing disease activity, joint swelling, and pain in patients with rheumatoid arthritis. It has also shown potential in reducing autoantibody production and improving lung function in patients with asthma. However, more research is needed to determine its full potential and efficacy in different types of autoimmune and inflammatory diseases.
Product mechanism: R406 works by binding to the ATP-binding site of the SYK kinase, preventing its activation and downstream signaling pathways that promote immune cell activation and inflammation. Its main targets include B-cell receptor (BCR), Fc receptors (FcR), and toll-like receptors (TLR), which are involved in the activation and maturation of B cells, mast cells, and macrophages. By inhibiting these receptors, R406 can block cytokine production and cellular activation, leading to reduced inflammation and tissue damage.
Safety: R406 has been evaluated in several clinical trials involving hundreds of patients with different autoimmune and inflammatory diseases. Overall, it has been well-tolerated, with manageable side effects. The most common adverse events reported were diarrhea, nausea, vomiting, fatigue, and headache. More severe side effects, such as infections and liver dysfunction, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of R406 include diarrhea, nausea, vomiting, fatigue, and headache. These symptoms are usually mild or moderate and can be managed with supportive care or dose modifications. Less common but more severe side effects may include infections and liver dysfunction. Patients should be monitored closely for these adverse events and receive appropriate medical intervention if necessary.
Dosing information: The recommended dose of R406 varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 50 to 1000 mg/day have been evaluated, either as a single agent or in combination with other drugs. Treatment duration also varies and can range from a few weeks to several months, depending on the response and tolerability. Patients should follow their doctor's instructions regarding dosing, administration, and monitoring.
Conclusion: SYK inhibitor R406 is a promising small-molecule inhibitor of the SYK kinase that has shown potential in preclinical and clinical studies for the treatment of various autoimmune and inflammatory diseases, such as rheumatoid arthritis, lupus, and asthma. Its mechanism of action involves blocking key receptors involved in immune cell activation and inflammation, leading to reduced disease activity and tissue damage. Although it has been generally well-tolerated, it may cause some side effects that should be monitored closely. Further research is needed to determine its full potential and efficacy in different types of autoimmune and inflammatory diseases.
