Antineoplastic agents targeting tyrosine kinases

Drugs that target tyrosine kinases belong to a new class of antineoplastic therapeutics, directed at cellular signalling mechanisms. Notes on the use of these agents and some of the clinical data are discussed in this review. The article is based on a review of recent literature and the authors' personal experience. Receptor tyrosine kinases and intracellular tyrosine kinases regulate cellular events that may be involved in tumour development, such as proliferation, survival, and angiogenesis. Some of these agents are established in clinical practice, in particular the small-molecular tyrosine kinase inhibitor imatinib in the treatment of chronic myeloid leukaemia and gastrointestinal stromal tumours and the antibody trastuzumab in the treatment of breast cancer. Inhibitors of epidermal growth factor receptor (EGFR) and other tyrosine kinases are either established in clinical practice or under clinical investigation.