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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 ...
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.
ALK inhibitors are anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation. [1] They fall under the category of tyrosine kinase inhibitors , which work by inhibiting proteins involved in the abnormal growth of tumour cells.
Intedanib is a multiple tyrosine kinase inhibitor and is the first drug to treat idiopathic pulmonary fibrosis. [4] Indol derivatives with 1-NH of 2-indolinone motif that is an H-bond donor, and 2-carbonyl oxygen that acts as an H-bond acceptor, bind with Glu915 and Cys917, respectively.
These inhibitors are used to treat cancers like non-small cell lung cancer, medullary thyroid carcinoma, and some types of colorectal and pancreatic cancer. RET inhibitors fall under the category of the tyrosine kinase inhibitors, which work by inhibiting proteins involved in the abnormal growth of cancer cells. Existing molecules fall in two ...
c-Met inhibitors are a class of small molecules that inhibit the enzymatic activity of the c-Met tyrosine kinase, the receptor of hepatocyte growth factor/scatter factor (HGF/SF). These inhibitors may have therapeutic application in the treatment of various types of cancers.
Lapatinib , used in the form of lapatinib ditosylate (trade names Tykerb and Tyverb marketed by Novartis) is an orally active drug for breast cancer and other solid tumours. [3] It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. [4]
Nilotinib is a Bcr-Abl tyrosine kinase inhibitor and works by interfering with signalling within the cancer cell. [3] [8] Nilotinib was approved for medical use in the United States in 2007. [3] [8] It is on the World Health Organization's List of Essential Medicines. [9] It is approved as a generic medication. [10]
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