Motesanib diphosphate (AMG706) (CAS: 857876-30-3) is a small-molecule inhibitor of multiple receptor tyrosine kinases, including vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and Kit, developed by Amgen for the treatment of various cancers, such as thyroid cancer and lung cancer. These receptors play a critical role in tumor angiogenesis and progression.
Chemical name: (2Z)-2-[[6,7-Dimethoxy-4-(2-pyrrolidin-1-ylethoxy)quinazolin-2-yl]imino]-5-[(phosphonooxy)methyl]phenol
Molecular formula: C22H28N4O9P
Formula weight: 520.45 g/mol
CAS No: 857876-30-3
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Health benefits of this product: Motesanib diphosphate has shown potential in preclinical and clinical studies for the treatment of various cancers, such as thyroid cancer and lung cancer. It works by inhibiting the activity of multiple receptor tyrosine kinases, which promote tumor angiogenesis and progression. By blocking these receptors, motesanib diphosphate can potentially reduce tumor growth and metastasis.
Potential effects: Motesanib diphosphate 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 thyroid cancer and lung cancer. 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: Motesanib diphosphate works by inhibiting the activity of multiple receptor tyrosine kinases, including VEGFR, PDGFR and Kit. These receptors are involved in the regulation of tumor angiogenesis and progression. Overexpression or mutation of these receptors is associated with various cancers, including thyroid cancer and lung cancer. As a tyrosine kinase inhibitor, motesanib diphosphate 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, motesanib diphosphate can block tumor progression and metastasis.
Safety: Motesanib diphosphate 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 hypertension, diarrhea, and fatigue. More severe side effects, such as cardiac toxicity and hemorrhage, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of motesanib diphosphate include hypertension, diarrhea, and fatigue. 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 cardiac toxicity and hemorrhage, 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 motesanib diphosphate varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 50 to 125 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: Motesanib diphosphate 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 thyroid cancer and lung cancer. 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.
