Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2014:2014:357027.
doi: 10.1155/2014/357027. Epub 2014 May 19.

Imatinib: a breakthrough of targeted therapy in cancer

Affiliations
Review

Imatinib: a breakthrough of targeted therapy in cancer

Nida Iqbal et al. Chemother Res Pract. 2014.

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.

PubMed Disclaimer

References

    1. Takimoto CH, Calvo E. Principles of oncological pharmacotherapy. In: Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ, editors. Cancer Management: A Multidisciplinary Approach. 11th edition 2008.
    1. Deininger MW, Druker BJ. Specific targeted therapy of chronic myelogenous leukemia with imatinib. Pharmacological Reviews. 2003;55(3):401–423. - PubMed
    1. Vigneri P, Wang JY. Induction of apoptosis in chronic myelogenous leukemia cells through nuclear entrapment of BCR-ABL tyrosine kinase. Nature Medicine. 2001;7(2):228–234. - PubMed
    1. Peng B, Dutreix C, Mehring G, et al. Absolute bioavailability of Imatinib (Glivec®) orally versus intravenous infusion. Journal of Clinical Pharmacology. 2004;44(2):158–162. - PubMed
    1. Peng B, Lloyd P, Schran H. Clinical pharmacokinetics of imatinib. Clinical Pharmacokinetics. 2005;44(9):879–894. - PubMed