Imatinib is a 2-phenyl amino pyrimidine derivative that functions as a tyrosine kinase inhibitor, including the Bcr-AbI pathway. It is an orally bioactive anti-cancer agent used in the treatment of cancers such as chronic myelogenous leukaemia (CML) and acute lymphocytic leukaemia (ALL), all of which are Philadelphia chromosome-positive (Ph+), as well as hypereosinophilic syndrome (HES) and certain types of gastrointestinal stromal tumours (GIST).
References
[1] Deininger MW. Milestones and monitoring in patients with CML treated with imatinib. Education Program Book; 50th ASH Conference; 2008. pp. 419–426.
[2] Druker BJ, Tamura S, Buchdunger E, Ohno S, Segal GM, Fanning S, Zimmermann J, Lydon NB. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med 1996. 1996;2:561–566. doi: 10.1038/nm0596-561.
[3] Deininger MW, Druker BJ: Specific targeted therapy of chronic myelogenous leukemia with imatinib. Pharmacol Rev. 2003 Sep;55(3):401-23. Epub 2003 Jul 1.
[4] Droogendijk HJ, Kluin-Nelemans HJ, van Doormaal JJ, Oranje AP, van de Loosdrecht AA, van Daele PL: Imatinib mesylate in the treatment of systemic mastocytosis: a phase II trial. Cancer. 2006 Jul 15;107(2):345-51.