Orantinib (SU6668) (CAS: 252916-29-3) is a small-molecule inhibitor of tyrosine kinases, including platelet-derived growth factor receptor (PDGFR), vascular endothelial growth factor receptor (VEGFR), and fibroblast growth factor receptor (FGFR), developed by SUGEN Inc. for the treatment of various cancers, such as renal cell carcinoma and glioblastoma. These receptors play a critical role in tumor angiogenesis and progression.
Chemical name: 3-[(2,4-dimethylpyrido[2,3-d]pyrimidin-7-yl)oxy]-5-methyl-N-methylpyrazine-2-carboxamide
Molecular formula: C18H19N5O2
Formula weight: 333.38 g/mol
CAS No: 252916-29-3
Top ten keywords from Google:
Synonyms:
Health benefits of this product: Orantinib has shown potential in preclinical and clinical studies for the treatment of various cancers, such as renal cell carcinoma and glioblastoma. It works by inhibiting the activity of several tyrosine kinases, including PDGFR, VEGFR, and FGFR, which promote tumor angiogenesis and progression. By blocking these receptors, orantinib can potentially reduce tumor growth and metastasis.
Potential effects: Orantinib 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 glioblastoma. 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: Orantinib inhibits the activity of several tyrosine kinases, including PDGFR, VEGFR, and FGFR, which are involved in the regulation of tumor angiogenesis and progression. Overexpression or activation of these receptors is associated with various cancers, such as renal cell carcinoma and glioblastoma. As a small-molecule inhibitor, orantinib 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, orantinib can block tumor progression and metastasis.
Safety: Orantinib 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, nausea, and diarrhea. More severe side effects, such as hypertension and thromboembolic events, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of orantinib include fatigue, nausea, and diarrhea. 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 thromboembolic events, 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 orantinib varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 10 to 200 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: Orantinib (SU6668) is a promising small-molecule inhibitor of PDGFR, VEGFR, and FGFR that has shown potential in preclinical and clinical studies for the treatment of various cancers, such as renal cell carcinoma and glioblastoma. 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.
