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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.
This is strong motivation to perform research on tyrosine kinase inhibitors as potential targets in cancer treatment. Gefitinib, functioning as an epidermal growth factor receptor tyrosine kinase inhibitor, improved symptoms related to non-small cell lung cancer and resulted in radiographic tumor regressions. [15]
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 ...
Lestaurtinib was identified early on as a trk receptor tyrosine kinase (RTK) inhibitor, with a concentration inhibiting 50% of tyrosine kinase activity (IC50) of 25 nM.In vivo trials demonstrated a 50–70% reduction in tumor burden for xenografted pancreatic and prostate cancers; however, subsequent clinical trials for pancreatic and prostate cancers did not achieve the endpoints specified.
Kinase inhibitors such as dasatinib are often used in the treatment of cancer and inflammation. [1] Some of the kinase inhibitors used in treating cancer are inhibitors of tyrosine kinases. [2] The effectiveness of kinase inhibitors on various cancers can vary from patient to patient. [3]
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.
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