Abstract
Deregulated protein tyrosine kinase activity is central to the pathogenesis of human cancers. Targeted therapy in the form of selective tyrosine kinase inhibitors (TKIs) has transformed the approach to management of various cancers and represents a therapeutic breakthrough. Imatinib was one of the first cancer therapies to show the potential for such targeted action. Imatinib, an oral targeted therapy, inhibits tyrosine kinases specifically BCR-ABL, c-KIT, and PDGFRA. Apart from its remarkable success in CML and GIST, Imatinib benefits various other tumors caused by Imatinib-specific abnormalities of PDGFR and c-KIT. Imatinib has also been proven to be effective in steroid-refractory chronic graft-versus-host disease because of its anti-PDGFR action. This paper is a comprehensive review of the role of Imatinib in oncology.
Highlights
Imatinib, a tyrosine kinase inhibitor, was called as “magical bullet,” when it revolutionized the treatment of chronic myeloid leukemia (CML) in 2001
The largest phase II study in patients with platelet-derived growth factor beta- (PDGFB-) positive advanced chordoma treated with Imatinib (800 mg daily) failed to elicit an overall tumour response defined by RECIST
Imatinib is the standard of care in CML and Gastrointestinal stromal tumors (GISTs) as it has dramatically changed the outlook of these diseases
Summary
Imatinib ( known as “Gleevec” or “Glivec”), a tyrosine kinase inhibitor, was called as “magical bullet,” when it revolutionized the treatment of chronic myeloid leukemia (CML) in 2001. Imatinib was invented in the late 1990s by biochemist Nicholas Lyndon working for Ciba-Geigy ( Novartis), and its use to treat CML was driven by Brian Druker, an oncologist at the Dana-Farber Institute. Druker, and the other colleagues were awarded the Lasker-DeBakey Clinical Medical Research Award in 2009 for “converting a fatal cancer into a manageable condition” and the Japan Prize in 2012 for their part in “the development of a new therapeutic drug targeting cancer-specific molecules.”. Encouraged by the success of Imatinib in treating CML patients, scientists explored its effect in other cancers and it was found to produce a similar miracle effect in other cancers where tyrosine kinases were overexpressed. This review discusses the clinical implications of Imatinib in various cancers
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