Rational drug design plays an important role in the development of new anticancer drugs. Target therapy is such a new antitumor treatment.
Imatinib (Glivec®) is an inhibitor of the protein-tyrosine kinase. This enzyme plays a major role in the signal transduction. It blocks kinases in the signal transduction of PDGF (platelet derived growth factor), SCF (stem cell factor), and c-kit.
By blocking this signal transduction, imatinib inhibits proliferation and even induces apoptosis. Imatinib also has effects in chronic myeloid leukemia. It has an application in the treatment of gastrointestinal stromal tumors (GIST) through PDGFR and c-KIT blockade. Adverse effects mostly involve headache, nausea, vomiting, diarrhea and dyspepsia.
I Imatinib interferes in the signal transduction.
II Imatinib treatment is relatively safe for the patient.
Extra info: The tyrosine kinase enzyme that is inhibited by imatinib, is a part of the signal transduction. Treatment with imatinib is only available for chronic myeloid leukemia patients with stemcell transplants. However, high morbidity and mortality occurs during the treatment. In this case α-interferon is the preferred treatment.