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Prostate cancer: Myelosuppression, diarrhoea, kidney failure, hypersensitivity, severe GI reactions (including perforation, ileus, colitis, etc.; all rare) and peripheral neuropathy Docetaxel: IV: As above. Breast cancer, non-small cell lung cancer, ovarian cancer, prostate cancer, squamous cell head and neck cancer and gastric cancer.
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.
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 ...
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.
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]
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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