VEGFR Tyrosine Kinase Inhibitor IV Tivozanib, also known as AV-951 or KRN-951, is a small molecule inhibitor that targets vascular endothelial growth factor receptors (VEGFRs) 1, 2, and 3. VEGFRs are transmembrane receptors that play a critical role in angiogenesis, or the formation of new blood vessels, which is essential for tumor growth and metastasis. Tivozanib has been shown to specifically inhibit VEGFRs, leading to the inhibition of angiogenesis and potentially providing a therapeutic benefit in cancer treatment.
Chemical Name and Molecular Formula:
The chemical name of Tivozanib is N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]thiazole-5-carboxamide. The molecular formula is C22H19ClN8O2S and the molecular weight is 500.95 g/mol.
CAS Number:
The CAS number for Tivozanib is 475108-18-0.
Top Ten Keywords and Synonyms:
Health Benefits of Tivozanib:
Tivozanib is currently being investigated as a potential cancer therapy due to its ability to inhibit angiogenesis. Angiogenesis is a complex process that involves the growth of new blood vessels from pre-existing ones. This process is essential for tumor growth and metastasis, as tumors require a blood supply to provide oxygen and nutrients to their cells. By inhibiting angiogenesis, Tivozanib may prevent the growth and spread of tumors.
Potential Effects of Tivozanib:
In preclinical studies, Tivozanib has been shown to effectively inhibit angiogenesis and tumor growth in animal models of cancer. In one study, Tivozanib was found to significantly reduce tumor growth in mice with implanted human renal cell carcinoma cells. Another study showed that Tivozanib inhibited VEGF-induced angiogenesis in rats, suggesting that it may have potential as an antiangiogenic agent in cancer therapy.
Product Mechanism:
Tivozanib acts by selectively binding to and inhibiting the activity of VEGFRs 1, 2, and 3, which are key regulators of angiogenesis. VEGFRs are expressed on the surface of endothelial cells, which line the inside of blood vessels. When the VEGF ligand binds to VEGFRs, a series of downstream signaling events are initiated that ultimately lead to endothelial cell proliferation, migration, and tube formation, all of which are necessary for angiogenesis. Tivozanib inhibits this process by preventing VEGFR phosphorylation and downstream signaling, resulting in reduced angiogenesis and potentially inhibiting tumor growth and metastasis.
Safety:
As with any drug, safety is a primary concern when investigating Tivozanib as a cancer therapy. While preclinical studies have shown promising results, further research is needed to determine the safety and efficacy of Tivozanib in humans. Additionally, like other VEGFR inhibitors, Tivozanib may cause adverse effects such as hypertension, proteinuria, and bleeding.
Side Effects:
In clinical trials, Tivozanib has been shown to cause adverse effects such as fatigue, diarrhea, and decreased appetite. Additionally, like other VEGFR inhibitors, Tivozanib may cause adverse effects such as hypertension, proteinuria, and bleeding.
Dosing Information:
Tivozanib is typically administered orally at a dose of 1.5 mg daily for 21 days followed by a 7-day break before the start of the next cycle. However, dosing may vary depending on the specific cancer being treated and the patient's individual characteristics.
Conclusion:
Tivozanib is a small molecule inhibitor that targets VEGFRs 1, 2, and 3, which play a critical role in angiogenesis, or the formation of new blood vessels. By inhibiting angiogenesis, Tivozanib may prevent the growth and spread of tumors, making it a promising candidate for cancer therapy. While further research is needed to determine the safety and efficacy of Tivozanib in humans, clinical trials have shown promising results, suggesting that it may have potential as a novel cancer therapy
