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A Method for Screening and Validation of Resistant Mutations Against Kinase Inhibitors
Published on: December 7, 2014
Imatinib: a breakthrough of targeted therapy in cancer
1Department of Medical Oncology, Dr. B. R. A. Institute Rotary Cancer Hospital, All India Institute of Medical Sciences, New Delhi 110029, India.
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.
Insights
Imatinib is a targeted cancer therapy drug that inhibits specific tyrosine kinases. It has shown success in treating chronic myeloid leukemia, gastrointestinal stromal tumors, and other cancers, transforming oncology treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Deregulated protein tyrosine kinase activity drives human cancer development.
- Selective tyrosine kinase inhibitors (TKIs) represent a breakthrough in cancer therapy.
- Imatinib was an early and successful example of targeted cancer therapy.
Purpose of the Study:
- To provide a comprehensive review of Imatinib's role in oncology.
- To highlight Imatinib's mechanism of action and therapeutic applications.
- To discuss Imatinib's impact on cancer management and other diseases.
Main Methods:
- Literature review of studies on Imatinib.
- Analysis of Imatinib's inhibitory targets (BCR-ABL, c-KIT, PDGFRA).
- Examination of clinical outcomes in various cancers and conditions.
Main Results:
- Imatinib demonstrates significant efficacy in chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GIST).
- The drug benefits other tumors with specific PDGFR and c-KIT abnormalities.
- Imatinib is effective in steroid-refractory chronic graft-versus-host disease due to its anti-PDGFR activity.
Conclusions:
- Imatinib is a crucial targeted therapy in oncology with broad applications.
- Its specific inhibition of key tyrosine kinases offers a paradigm shift in cancer treatment.
- Imatinib's success underscores the potential of targeted therapies in managing complex diseases.
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