Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Imatinib

Living reference work entry
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DOI: https://doi.org/10.1007/978-3-642-27841-9_2963-2
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Synonyms

CGP57148; Imatinib mesylate; STI571; STI-571

Definition

It is a small molecular weight compound that inhibits tyrosine kinases including ABL, KIT (Kit/stem cell factor receptor in oncogenesis), and PDGFR (platelet-derived growth factor receptor). It has significant antitumor activity in chronic myeloid leukemia (CML) and gastrointestinal stromal tumors.

Characteristics

Imatinib (US brand name: Gleevec, foreign brand name: Glivec, formerly STI571 or CGP57148) is a tyrosine kinase inhibitor with activity against all of the ABL tyrosine kinases including BCR-ABL1, ABL, v-ABL, and ARG (Abelson-related gene). Besides the ABL tyrosine kinase, other kinases inhibited by imatinib are the platelet-derived growth factor receptor alpha (PDGFRA) and beta (PDGFRB) and KIT. Given the critical role of receptor tyrosine kinasesin the regulation of cellular growth and known activating mutations that cause several cancers, it was hypothesized that specific inhibitors of these protein kinases...

Keywords

Chronic Myeloid Leukemia Gastrointestinal Stromal Tumor Chronic Myeloid Leukemia Patient Blast Crisis Chronic Myeloid Leukemia Cell 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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References

  1. Druker BJ (2006) Circumventing resistance to kinase-inhibitor therapy. N Engl J Med 354:2594–2596CrossRefPubMedGoogle Scholar
  2. Druker BJ, Tamura S, Buchdunger E et al (1996) Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med 2:561–566CrossRefPubMedGoogle Scholar
  3. Druker BJ, Talpaz M, Resta DJ et al (2001) Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med 344:1031–1037CrossRefPubMedGoogle Scholar
  4. Druker BJ, Guilhot F, O’Brien SG et al (2006) Five-year follow- up of patients receiving imatinib for chronic myeloid leukemia. N Engl J Med 355:2408–2417CrossRefPubMedGoogle Scholar
  5. Heinrich MC, Corless CL, Demetri GD et al (2003) Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol 21:4342–4349CrossRefPubMedGoogle Scholar

See Also

  1. (2012) ABL. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 14. doi: 10.1007/978-3-642-16483-5_15Google Scholar
  2. (2012) Dasatinib. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 1060. doi: 10.1007/978-3-642-16483-5_1518Google Scholar
  3. (2012) Dermatofibrosarcoma Protuberans. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 1087. doi: 10.1007/978-3-642-16483-5_7044Google Scholar
  4. (2012) Exon. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 1360. doi: 10.1007/978-3-642-16483-5_2059Google Scholar
  5. (2012) FDA. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 1386. doi: 10.1007/978-3-642-16483-5_2136Google Scholar
  6. (2012) KIT. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, pp 1945–1946. doi: 10.1007/978-3-642-16483-5_3228Google Scholar
  7. (2012) Mutation. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 2412. doi: 10.1007/978-3-642-16483-5_3911Google Scholar
  8. (2012) Pharmacodynamics. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 2840. doi: 10.1007/978-3-642-16483-5_4495Google Scholar
  9. (2012) Pharmacokinetics. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 2845. doi: 10.1007/978-3-642-16483-5_4500Google Scholar
  10. (2012) Philadelphia Chromosome. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 2864. doi: 10.1007/978-3-642-16483-5_4520Google Scholar
  11. (2012) Platelet-Derived Growth Factor Receptor. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 2910. doi: 10.1007/978-3-642-16483-5_4612Google Scholar
  12. (2012) Reciprocal Translocation. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 3204. doi: 10.1007/978-3-642-16483-5_4989Google Scholar
  13. (2012) Sunitinib. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 3562. doi: 10.1007/978-3-642-16483-5_5575Google Scholar
  14. (2012) Tyrosine Kinase. In: Schwab M (ed) Encyclopedia of Cancer, 3rd edn. Springer Berlin Heidelberg, p 3822. doi: 10.1007/978-3-642-16483-5_6079Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  1. 1.Oregon Health & Science University Cancer InstitutePortlandUSA