Bafetinib (INNO-406) (CAS: 859212-16-1) is a small-molecule inhibitor of tyrosine kinases, developed by InnoPharma for the treatment of various cancers, such as chronic myeloid leukemia (CML). Tyrosine kinases play a critical role in cell proliferation and survival.
Chemical name: 5-[(3-chloro-4-methylphenyl)amino]-2-fluoro-N-[(2-hydroxyethoxy)methyl]benzamide
Molecular formula: C22H23ClFN3O3
Formula weight: 441.89 g/mol
CAS No: 859212-16-1
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Health benefits of this product: Bafetinib has shown potential in preclinical and clinical studies for the treatment of various cancers, particularly chronic myeloid leukemia. It works by inhibiting the activity of several tyrosine kinases, which are involved in cell proliferation and survival. By blocking these receptors, bafetinib can potentially induce apoptosis and inhibit tumor growth.
Potential effects: Bafetinib has demonstrated efficacy in reducing tumor growth and inducing remission in chronic myeloid leukemia in preclinical and clinical studies. It has also shown potential in combination with other anti-cancer agents, such as chemotherapy and radiation therapy. However, more research is needed to determine its full potential and efficacy in different types of cancers.
Product mechanism: Bafetinib inhibits the activity of several tyrosine kinases, including BCR-ABL, Lyn, and Fyn, which are involved in cell proliferation and survival. Overexpression or activation of these receptors is associated with various cancers, particularly chronic myeloid leukemia. As a small-molecule inhibitor, bafetinib binds to the ATP-binding site of these receptors, preventing their activation and downstream signaling pathways that promote cancer cell growth and survival. By inhibiting these receptors, bafetinib can induce apoptosis and inhibit tumor growth.
Safety: Bafetinib has been evaluated in several preclinical and clinical studies involving hundreds of patients with different types of cancers. Overall, it has been well-tolerated, with manageable side effects. The most common adverse events reported were fatigue, diarrhea, and nausea. More severe side effects, such as liver toxicity and QT prolongation, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of bafetinib include fatigue, diarrhea, and nausea. 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 liver toxicity and QT prolongation, which may require prompt medical intervention. Patients should be monitored closely for these adverse events and receive appropriate medical intervention if necessary.
Dosing information: The recommended dose of bafetinib varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 50 to 400 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: Bafetinib (INNO-406) is a promising small-molecule inhibitor of tyrosine kinases that has shown potential in preclinical and clinical studies for the treatment of various cancers, particularly chronic myeloid leukemia. Its mechanism of action involves blocking key receptors involved in cell proliferation and survival, leading to apoptosis and reduced tumor growth. 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 cancers