Brivanib alaninate (CAS: 649735-63-7) is a small-molecule inhibitor of vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) developed by Bristol-Myers Squibb for the treatment of various cancers, such as hepatocellular carcinoma (HCC) and metastatic colorectal cancer (mCRC). VEGFR and FGFR are key receptors involved in angiogenesis, or the formation of new blood vessels, which is essential for tumor growth and metastasis.
Chemical name: (2S)-2-(3-(4-(((2-amino-4-chloro-5-fluorophenyl)amino)methyl)piperidin-1-yl)-2-hydroxypropoxy)propanoic acid ethyl ester
Molecular formula: C23H34ClFN4O4
Formula weight: 495.99 g/mol
CAS No: 649735-63-7
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Health benefits of this product: Brivanib alaninate has shown potential in preclinical and clinical studies for the treatment of various cancers, such as HCC and mCRC. It works by inhibiting the activity of VEGFR and FGFR, which promote tumor growth and angiogenesis. By blocking these receptors, brivanib alaninate can potentially reduce tumor progression and metastasis.
Potential effects: Brivanib alaninate 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 HCC and mCRC. 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: Brivanib alaninate works by inhibiting the activity of VEGFR and FGFR, which are involved in the regulation of angiogenesis and tumor growth. Overexpression of these receptors is associated with various cancers, including HCC and mCRC. As a tyrosine kinase inhibitor, brivanib alaninate binds to the ATP-binding site of VEGFR and FGFR, preventing their activation and downstream signaling pathways that promote cancer cell growth and angiogenesis. By inhibiting VEGFR and FGFR, brivanib alaninate can block tumor growth and induce apoptosis.
Safety: Brivanib alaninate 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, hypertension, diarrhea, and nausea. More severe side effects, such as thromboembolism and liver toxicity, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of brivanib alaninate include fatigue, hypertension, 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 thromboembolism and liver 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 brivanib alaninate varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 200 to 800 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: Brivanib alaninate is a promising small-molecule inhibitor of VEGFR and FGFR that has shown potential in preclinical and clinical studies for the treatment of various cancers, such as HCC and mCRC
