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Updated: Aug 13, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
Src tyrosine kinase as a chemotherapeutic target: is there a clinical case?
Ting Chen1, Jessica A George, Christopher C Taylor
1Department of Cell Biology, Vincent T. Lombardi Comprehensive Cancer Center, Georgetown University School of Medicine, Washington, District of Columbia 20007, USA.
Abstract:
Src tyrosine kinase was the first protooncogene described. It has been found to be overexpressed and activated in a large number of different cancers. Cellular Src has been shown to activate a number of different effectors that are involved in different aspects of cancer biology such as metastasis, cell cycle regulation and cell survival. Despite this, Src inhibitors have not entered the regular arsenal of chemotherapeutics. This article reviews some of the biology, rationale, in vitro and in vivo preclinical evidence, and some very early clinical trials demonstrating efficacy of Src inhibitors.
Insights
Src tyrosine kinase (proto-oncogene) is often overexpressed in cancers, driving metastasis and survival. This review covers Src inhibitor biology, preclinical data, and early clinical trials showing potential efficacy.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Src tyrosine kinase is a proto-oncogene implicated in numerous cancers.
- Its overexpression and activation correlate with cancer progression, including metastasis, cell cycle dysregulation, and enhanced cell survival.
- Despite its role in cancer, Src inhibitors are not standard chemotherapeutics.
Purpose of the Study:
- To review the biological underpinnings of Src tyrosine kinase in cancer.
- To examine the rationale for developing Src inhibitors.
- To present preclinical and early clinical evidence for Src inhibitor efficacy.
Main Methods:
- Literature review of Src biology and cancer association.
- Analysis of in vitro and in vivo preclinical studies on Src inhibitors.
- Summary of findings from early-phase clinical trials of Src inhibitors.
Main Results:
- Src tyrosine kinase plays a significant role in multiple cancer hallmarks.
- Preclinical studies demonstrate the anti-cancer potential of Src inhibitors.
- Early clinical trials suggest promising efficacy, warranting further investigation.
Conclusions:
- Src tyrosine kinase is a validated cancer target.
- Src inhibitors show therapeutic promise, supported by preclinical and early clinical data.
- Further clinical development of Src inhibitors is justified for cancer treatment.
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