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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 ...
Inhibitors of tyrosine kinase are mainly used against some specific forms of cancer. Subcategories. This category has the following 2 subcategories, out of 2 total. ...
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.
Kinase inhibitors such as dasatinib are often used in the treatment of cancer and inflammation. [4] Some of the kinase inhibitors used in treating cancer are inhibitors of tyrosine kinases. [5] The effectiveness of kinase inhibitors on various cancers can vary from patient to patient. [6]
Approved drugs that inhibit BTK: Ibrutinib (Imbruvica), a selective Bruton's tyrosine kinase inhibitor. Acalabrutinib (Calquence), approved in October 2017 [16] for relapsed mantle cell lymphoma and in October 2019 for Chronic lymphocytic leukemia (CLL) and Small lymphocytic lymphoma (SLL)
Later, series of more selective c-Met inhibitors were designed, where an indolin-2-one core (encircled in figure 1) was present in several kinase inhibitors. SU-11274 was evolved by substitution at the 5-position of the indolinone [ 9 ] and by adding a 3,5-dimethyl pyrrole group, PHA-665752 was evolved [ 11 ] – a second-generation inhibitor ...
5.10 L01EK Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors 5.11 L01EL Bruton's tyrosine kinase (BTK) inhibitors 5.12 L01EM Phosphatidylinositol-3-kinase (Pi3K) inhibitors