[Antineoplastic agents targeting tyrosine kinases].
BACKGROUND
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.


METHODS
The article is based on a review of recent literature and the authors' personal experience.


CONCLUSIONS
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.
Guren
Tormod K
TK
Farmakologisk institutt, Rikshospitalet, Universitetet i Oslo, Postboks 1057 Blindern, 0316 Oslo. t.k.guren@medisin.uio.no
Christoffersen
Thoralf
T
Thoresen
G Hege
GH
Wisløff
Finn
F
Dajani
Olav
O
Tveit
Kjell M
KM
D000911:Antibodies, Monoclonal / Q000008:administration & dosage / Q000627:therapeutic use*; D061067:Antibodies, Monoclonal, Humanized; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000627:therapeutic use*; D001549:Benzamides; D000068818:Cetuximab; D066246:ErbB Receptors / Q000037:antagonists & inhibitors / Q000276:immunology; D000069347:Erlotinib Hydrochloride; D046152:Gastrointestinal Stromal Tumors / Q000188:drug therapy / Q000201:enzymology / Q000276:immunology; D000077156:Gefitinib; D006801:Humans; D000068877:Imatinib Mesylate; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy / Q000201:enzymology / Q000276:immunology; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000276:immunology; D010879:Piperazines / Q000008:administration & dosage / Q000627:therapeutic use; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000276:immunology; D011743:Pyrimidines / Q000008:administration & dosage / Q000627:therapeutic use; D011799:Quinazolines / Q000008:administration & dosage / Q000627:therapeutic use; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors / Q000276:immunology; D017479:Receptors, Platelet-Derived Growth Factor / Q000037:antagonists & inhibitors / Q000276:immunology; D015398:Signal Transduction / Q000187:drug effects; D000068878:Trastuzumab
D000911:Antibodies, Monoclonal; D061067:Antibodies, Monoclonal, Humanized; D000970:Antineoplastic Agents; D001549:Benzamides; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D011799:Quinazolines; D000068877:Imatinib Mesylate; D000069347:Erlotinib Hydrochloride; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases; D020794:Receptor Protein-Tyrosine Kinases; D017479:Receptors, Platelet-Derived Growth Factor; C485206:pertuzumab; D000068878:Trastuzumab; D000068818:Cetuximab; D000077156:Gefitinib