Varlitinib (ARRY334543, CAS: 845272-21-1) is a small-molecule inhibitor of the epidermal growth factor receptor (EGFR) and HER2 tyrosine kinases developed by Array BioPharma for the treatment of various types of cancer. It was designed to overcome some of the limitations and resistance mechanisms of other EGFR and HER2 inhibitors, such as erlotinib and lapatinib.
Chemical name: 4-(4-{[4-chloro-3-(trifluoromethyl)phenyl]amino}-7-methoxyquinazolin-6-yl)-N-ethylpiperazine-1-carboxamide
Molecular formula: C24H25ClF3N5O2
Formula weight: 507.93 g/mol
CAS No: 845272-21-1
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Health benefits of this product: Varlitinib has shown potential in preclinical and clinical studies for the treatment of different types of cancer, including non-small cell lung cancer (NSCLC), gastric cancer, breast cancer, and colorectal cancer. It works by inhibiting the activity of the EGFR and HER2 receptors, which are involved in tumor growth and progression. By blocking these receptors, Varlitinib can potentially reduce cancer cell proliferation, migration, and invasion, leading to decreased tumor growth and metastasis.
Potential effects: Varlitinib has shown promising antitumor activity in preclinical studies and clinical trials. In particular, it has demonstrated efficacy in patients with HER2-positive cancers, such as gastric cancer and breast cancer, where other HER2 inhibitors have failed. It has also shown potential as a combination therapy with other anticancer agents, such as paclitaxel and ramucirumab. However, more research is needed to determine its full potential and efficacy in different types of cancer.
Product mechanism: Varlitinib works by binding to the ATP-binding site of the EGFR and HER2 receptors, preventing their activation and downstream signaling pathways that promote tumor growth and progression. Its main targets include the tyrosine kinase domains of both receptors, which are crucial for their dimerization and activation. By inhibiting these receptors, Varlitinib can block cell survival and proliferation signals, leading to apoptosis (programmed cell death) and reduced tumor growth and metastasis.
Safety: Varlitinib has been evaluated in several clinical trials involving hundreds of patients with different types of cancer. Overall, it has been well-tolerated, with manageable side effects. The most common adverse events reported were diarrhea, nausea, vomiting, fatigue, and skin rash. More severe side effects, such as hypertension, liver dysfunction, and neutropenia, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of Varlitinib include diarrhea, nausea, vomiting, fatigue, and skin 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, liver dysfunction, and neutropenia. Patients should be monitored closely for these adverse events and receive appropriate medical intervention if necessary.
Dosing information: The recommended dose of Varlitinib varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 300 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: Varlitinib is a promising small-molecule inhibitor of the EGFR and HER2 tyrosine kinases that has shown potential in preclinical and clinical studies for the treatment of different types of cancer. Its mechanism of action involves blocking key receptors involved in cancer cell growth and metastasis, leading to reduced tumor progression. 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 cancer.
