Linsitinib (CAS: 867160-71-2) is a small-molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R), developed by OSI Pharmaceuticals for the treatment of various cancers, such as breast cancer and non-small cell lung cancer. IGF-1R plays a critical role in tumor growth and survival.
Chemical name: N-[2-hydroxy-4-methyl-5-(2-methylpropyl)phenyl]-4-[(4-methyl-2-quinolinyl)amino]-1-piperidinecarboxamide
Molecular formula: C27H32N4O3
Formula weight: 452.57 g/mol
CAS No: 867160-71-2
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Health benefits of this product: Linsitinib has shown potential in preclinical and clinical studies for the treatment of various cancers, particularly breast cancer and non-small cell lung cancer. It works by inhibiting the activity of IGF-1R, which is involved in tumor growth and survival. By blocking these receptors, linsitinib can potentially induce apoptosis and inhibit tumor growth.
Potential effects: Linsitinib has demonstrated efficacy in reducing tumor growth and inducing remission in breast cancer and non-small cell lung cancer in preclinical and clinical studies. 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: Linsitinib inhibits the activity of IGF-1R, which is involved in tumor growth and survival. Activation of this receptor by insulin-like growth factors (IGFs) promotes cell proliferation, survival, and migration, leading to tumor growth and metastasis. As a small-molecule inhibitor, linsitinib binds to the ATP-binding site of IGF-1R, preventing its activation and downstream signaling pathways that promote cancer cell growth and survival. By inhibiting these receptors, linsitinib can induce apoptosis and inhibit tumor growth.
Safety: Linsitinib 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 hyperglycemia, fatigue, and diarrhea. More severe side effects, such as liver toxicity and thrombocytopenia, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of linsitinib include hyperglycemia, fatigue, 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 liver toxicity and thrombocytopenia, 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 linsitinib varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 30 to 150 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: Linsitinib (CAS: 867160-71-2) is a promising small-molecule inhibitor of IGF-1R that has shown potential in preclinical and clinical studies for the treatment of various cancers, particularly breast cancer and non-small cell lung cancer. Its mechanism of action involves blocking key receptors involved in tumor growth and survival, leading to apoptosis and reduced tumor growth. 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.
