Dovitinib (TKI-258, CHIR-258) (CAS: 405169-16-6) is a small-molecule inhibitor of multiple receptor tyrosine kinases, including fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor (VEGFR), and platelet-derived growth factor receptor (PDGFR), developed by Novartis for the treatment of various cancers, such as renal cell carcinoma and gastrointestinal stromal tumors. These receptors play a critical role in tumor angiogenesis and progression.
Chemical name: N-(2,4-dimethyl-5-(5-((trifluoromethyl)sulfonyl)pyridin-2-ylamino)phenyl)-4-((2-oxoindolin-3-ylidene)methyl)piperazine-1-carboxamide
Molecular formula: C26H28F3N7O4S
Formula weight: 569.61 g/mol
CAS No: 405169-16-6
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Health benefits of this product: Dovitinib has shown potential in preclinical and clinical studies for the treatment of various cancers, such as renal cell carcinoma and gastrointestinal stromal tumors. It works by inhibiting the activity of multiple receptor tyrosine kinases, which promote tumor angiogenesis and progression. By blocking these receptors, dovitinib can potentially reduce tumor growth and metastasis.
Potential effects: Dovitinib has shown promising anti-tumor activity in preclinical and clinical studies. In particular, it has demonstrated efficacy in reducing tumor growth and inducing remission in renal cell carcinoma and gastrointestinal stromal tumors. 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 tumors.
Product mechanism: Dovitinib works by inhibiting the activity of multiple receptor tyrosine kinases, including FGFR, VEGFR, and PDGFR. These receptors are involved in the regulation of tumor angiogenesis and progression. Overexpression or mutation of these receptors is associated with various cancers, including renal cell carcinoma and gastrointestinal stromal tumors. As a tyrosine kinase inhibitor, dovitinib binds to the ATP-binding site of these receptors, preventing their activation and downstream signaling pathways that promote cancer cell growth and metastasis. By inhibiting these receptors, dovitinib can block tumor progression and metastasis.
Safety: Dovitinib 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 hypertension and cardiac toxicity, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of dovitinib 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 hypertension and cardiac toxicity, 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 dovitinib varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 100 to 500 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: Dovitinib is a promising small-molecule inhibitor of multiple receptor tyrosine kinases that has shown potential in preclinical and clinical studies for the treatment of various cancers, such as renal cell carcinoma and gastrointestinal stromal tumors. Its mechanism of action involves blocking key receptors involved in tumor angiogenesis and progression, leading to reduced tumor growth and metastasis. 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
