n. a *cytotoxic drug that works by inhibiting tyrosine kinases, enzymes that are active in some cancer cells (see tyrosine kinase inhibitor). Imatinib is used in the treatment of chronic myeloid leukaemia in which the *Philadelphia chromosome is present, *myeloproliferative disorders associated with abnormalities of the platelet-derived growth factor receptor gene, *gastrointestinal stromal tumours (GIST), and acute lymphoblastic leukaemia. The commonest side-effects are intestinal upset, fluid retention, and muscle pain and cramps.
n. an inhibitor of multiple kinases (see protein kinase; tyrosine kinase inhibitor) that blocks the action of *vascular endothelial growth factor. It is used for the treatment of advanced *renal cell carcinoma and of *gastrointestinal stromal tumour after disease progression or on intolerance to *imatinib. Its most common side-effects include fatigue, asthenia, gastrointestinal disturbances, hypertension, and bleeding.... sunitinib
(targeted therapy) a drug that interferes with specific molecular targets in the pathways involved in cancer cell growth and signalling, in contrast to *cytotoxic drugs that act primarily on rapidly dividing cells. It typically requires prolonged courses of treatment, and the anticancer action can be synergistic with *chemotherapy. Many new drugs are being developed and are undergoing trials to determine optimal use. The *tyrosine kinase inhibitors include imatinib and *epidermal growth factor receptor inhibitors; multitargeted agents include *sorafenib and *sunitinib. The monoclonal antibodies include *rituximab, *trastuzumab, *cetuximab, and *bevacizumab.... targeted agent
any one of a class of drugs that interfere with cell growth in a variety of different ways by inhibiting the action of tyrosine kinases. This family of enzymes, which occur both within cells and as components of cell-membrane receptor sites, have an important role in cell division and cell growth. Many tumour cells have been shown to have both intracellular enzymes and extracellular receptor sites, and a variety of anticancer agents have been developed to inhibit enzyme activity at these sites. Among these drugs are *imatinib, dasatinib, and nilotinib, used for treating chronic myeloid leukaemia; *sunitinib, for treating renal cell carcinoma; and erlotinib, for treating pancreatic cancer and non-small-cell lung cancer. See also epidermal growth factor receptor.... tyrosine kinase inhibitor
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