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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 ...
Imatinib use may cause lightening/depigmentation or darkening/repigmentation of hair (as is the case with some other tyrosine kinase inhibitors) and/or skin as well as hyperpigmentation of the gingiva. The median onset of hair color change is 4 weeks after initiation of therapy (but may occur over a year after initiation), is dose-dependent ...
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.
Angiogenesis inhibitors such as nintedanib may be effective in a range of solid tumour types including lung, ovarian, metastatic bowel, liver and brain cancer. [ medical citation needed ] Current [ when? ] phase II trials are investigating the effect of nintedanib in patients with bladder cancer, metastatic bowel cancer, liver cancer and the ...
Ceritinib is an anaplastic lymphoma kinase (ALK) inhibitor primarily used for the treatment of ALK positive metastatic NSCLC. [8] [9] Previously, it was only indicated for patients who had developed resistant to crizotinib, another ALK inhibitor, but has since had its usage expanded to serve as a primary option for metastatic NSCLC.
Gefitinib is a tyrosine kinase inhibitor that targets the epidermal growth factor receptor, inducing favorable outcomes in patients with non-small cell lung cancers. A common, widespread cancer, non-small cell lung cancer is the cause of death in more people than breast, colorectal, and prostate cancer together. [ 15 ]
Cediranib (AZD-2171; tentative trade name Recentin) is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases. [1] [2] [3] The drug is being developed by AstraZeneca as a possible anti-cancer chemotherapeutic agent for oral administration.
National Cancer Institute. "Crizotinib". National Cancer Institute. 11 October 2011. Clinical trial number NCT00585195 for "A Study Of Oral PF-02341066, A C-Met/Hepatocyte Growth Factor Tyrosine Kinase Inhibitor, In Patients With Advanced Cancer (PROFILE 1001)" at ClinicalTrials.gov