AEE788 (NVP-AEE788, CAS: 497839-62-0) is a small-molecule inhibitor of epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) developed by Novartis for the treatment of various cancers, such as glioblastoma multiforme (GBM) and non-small cell lung cancer (NSCLC). EGFR and VEGFR are key receptors involved in tumor cell proliferation, survival, and angiogenesis.
Chemical name: N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)acrylamide
Molecular formula: C24H22ClFN4O3
Formula weight: 466.9 g/mol
CAS No: 497839-62-0
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Health benefits of this product: AEE788 has shown potential in preclinical and clinical studies for the treatment of various cancers, such as GBM and NSCLC. It works by inhibiting the activity of EGFR and VEGFR, which promote tumor growth and angiogenesis. By blocking these receptors, AEE788 can potentially reduce tumor progression and metastasis.
Potential effects: AEE788 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 GBM and NSCLC. 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: AEE788 works by inhibiting the activity of EGFR and VEGFR, which are involved in the regulation of tumor cell proliferation, survival, and angiogenesis. Overexpression of these receptors is associated with various cancers, including GBM and NSCLC. As a tyrosine kinase inhibitor, AEE788 binds to the ATP-binding site of EGFR and VEGFR, preventing their activation and downstream signaling pathways that promote cancer cell growth and angiogenesis. By inhibiting EGFR and VEGFR, AEE788 can block tumor growth and induce apoptosis.
Safety: AEE788 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, nausea, and rash. More severe side effects, such as hypertension and arterial thrombosis, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of AEE788 include fatigue, diarrhea, nausea, and rash. 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 arterial thrombosis, 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 AEE788 varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 100 to 600 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: AEE788 is a promising small-molecule inhibitor of EGFR and VEGFR that has shown potential in preclinical and clinical studies for the treatment of various cancers, such as GBM and NSCLC. Its mechanism of action involves blocking key receptors involved in tumor growth and angiogenesis, leading to reduced tumor progression 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
