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Repotrectinib is indicated for the treatment of adults with locally advanced or metastatic ROS1-positive non-small cell lung cancer. [1] [2]In June 2024, the US Food and Drug Administration (FDA) expanded the indication to include the treatment of people twelve years of age and older with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion, are locally advanced or ...
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.
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 ...
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]
Dasatinib is an ATP-competitive protein tyrosine kinase inhibitor. The main targets of dasatinib are BCR/Abl (the "Philadelphia chromosome"), Src, c-Kit, ephrin receptors, and several other tyrosine kinases. [12] Strong inhibition of the activated BCR-ABL kinase distinguishes dasatinib from other CML treatments, such as imatinib and nilotinib.
The tablets are formulated as fostamatinib disodium hexahydrate, a disodium hexahydrate salt, and is a prodrug of the active compound tamatinib (R-406), [7] which is an inhibitor of the enzyme spleen tyrosine kinase (Syk), [8] hence it is an syk inhibitor. Syk is a protein tyrosine kinase associated with various inflammatory cells, including ...
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Osimertinib, sold under the brand name Tagrisso, [6] is a medication used to treat non-small-cell lung carcinomas with specific mutations. [7] [8] It is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor.
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