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A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation), a step that TKIs inhibit. TKIs are typically used as ...
It is a multi-targeted tyrosine-kinase inhibitor. [5] Some forms of chronic myeloid leukemia, those that have the T315I mutation, are resistant to current therapies such as imatinib. Ponatinib has been designed to be effective against these types of tumors. [6] Ponatinib was approved for medical use in the United States in December 2012. [7]
Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR: Medullary thyroid cancer. Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). 2.3 mTOR inhibitors: Everolimus: PO: mTOR inhibitor.
Tyrosine kinase activity in the nucleus involves cell-cycle control and properties of transcription factors. [3] In this way, in fact, tyrosine kinase activity is involved in mitogenesis, or the induction of mitosis in a cell; proteins in the cytosol and proteins in the nucleus are phosphorylated at tyrosine residues during this process. [3]
Gefitinib is the first selective inhibitor of epidermal growth factor receptor's (EGFR) tyrosine kinase domain. Thus gefitinib is an EGFR inhibitor.The target protein (EGFR) is a member of a family of receptors which includes Her1(EGFR), Her2(erb-B2), Her3(erb-B3) and Her4 (Erb-B4).
Tivozanib, sold under the brand name Fotivda, is a medication used for the treatment of advanced renal cell carcinoma (kidney cancer). [3] It is an oral VEGF receptor tyrosine kinase inhibitor.
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