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.
an enzyme that catalyses the transfer of a phosphate group from ATP to a specific amino acid residue of an intracellular protein (usually serine, threonine, or tyrosine), thereby affecting the biological activity of the protein. Protein kinase inhibitors are drugs that block the action of protein kinases in tumour cells and are used in the treatment of cancer. They include *sorafenib, *sunitinib, and *temsirolimus. See also tyrosine kinase inhibitor.... protein kinase
(Grawitz tumour, hypernephroma) a malignant tumour of kidney cells (the alternative name refers to its supposed resemblance to part of the adrenal gland and at one time it was thought to originate from this site). It may be present for some years before giving rise to symptoms, which include fever, loin pain and swelling, and blood in the urine. Treatment is by surgery, but tumours are apt to recur locally or spread via the bloodstream and can often be seen growing along the renal vein. Secondary growths from a renal cell carcinoma in the lung have a characteristic ‘cannon-ball’ appearance. These tumours are relatively insensitive to radiotherapy and cytotoxic drugs but some respond to such hormones as progestogens. Targeted therapy with *sorafenib and *sunitinib has significantly changed the treatment of advanced tumours.... renal cell carcinoma
(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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