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Updated: Jun 12, 2025

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
A review on tyrosine kinase inhibitors for targeted breast cancer therapy
Vidya Sankarapandian1, Ramya Lakshmi Rajendran2, Conrad Ondieki Miruka3
1Department of Microbiology and Immunology, Kampala International University, Western Campus, Box 20000, Uganda.
Abstract:
Breast cancer is a heterogeneous disease with complex molecular pathogenesis. Overexpression of several tyrosine kinase receptors is associated with poor prognosis, therefore, they can be key targets in breast cancer therapy. Tyrosine kinase inhibitors (TKIs) have emerged as leading agents in targeted cancer therapy due to their effectiveness in disrupting key molecular pathways involved in tumor growth. TKIs target various tyrosine kinases, including the human epidermal growth factor receptor 2 (HER2), epidermal growth factor receptor (EGFR), Vascular endothelial growth factor receptor (VEGFR), anaplastic lymphoma kinase (ALK), vascular endothelial growth factor receptor (VEGFR)-associated multi-targets, rearranged during transfection (RET), fibroblast growth factor receptor (FGFR), receptor tyrosine kinase-like orphan signal 1 (ROS1), Mitogen-activated protein kinase (MAPK), and tropomyosin receptor kinase (TRK). These drugs target the tyrosine kinase domain of receptor tyrosine kinases and play a vital role in proliferation and migration of breast cancer cells. Several TKIs, including lapatinib, neratinib, and tucatinib, have been developed and are currently used in clinical settings, often in combination with chemotherapy, endocrine therapy, or other targeted agents. TKIs have demonstrated remarkable benefits in enhancing progression-free and overall survival in patients with breast cancer and have become a standard of care for this population. This review provides an overview of TKIs currently being examined in preclinical studies and clinical trials, especially in combination with drugs approved for breast cancer treatment. TKIs have emerged as a promising therapeutic option for patients with breast cancer and hold potential for treating other breast cancer subtypes. The development of new TKIs and their integration into personalized treatment strategies will continue to shape the future of breast cancer therapy.
Insights
Tyrosine kinase inhibitors (TKIs) are effective targeted therapies for breast cancer, disrupting tumor growth pathways. This review explores TKIs in clinical trials, showing improved survival and potential for personalized breast cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Breast cancer is a complex disease with molecular heterogeneity.
- Overexpressed tyrosine kinase receptors are linked to poor prognosis, making them therapeutic targets.
- Tyrosine kinase inhibitors (TKIs) disrupt key pathways in tumor growth and proliferation.
Purpose of the Study:
- To review current and emerging tyrosine kinase inhibitors (TKIs) for breast cancer treatment.
- To explore the role of TKIs in preclinical studies and clinical trials.
- To discuss the integration of TKIs into personalized breast cancer therapy.
Main Methods:
- Literature review of preclinical studies and clinical trials on TKIs in breast cancer.
- Analysis of TKI mechanisms targeting receptor tyrosine kinases (e.g., HER2, EGFR, VEGFR).
- Examination of TKI efficacy when used in combination with chemotherapy, endocrine therapy, or other targeted agents.
Main Results:
- TKIs targeting various tyrosine kinases (HER2, EGFR, VEGFR, ALK, RET, FGFR, ROS1, MAPK, TRK) are crucial in breast cancer.
- Approved TKIs like lapatinib, neratinib, and tucatinib improve progression-free and overall survival.
- TKIs show promise as a therapeutic option for various breast cancer subtypes.
Conclusions:
- TKIs represent a significant advancement in targeted breast cancer therapy.
- Combination therapies involving TKIs enhance patient outcomes.
- Future breast cancer treatment will likely involve novel TKIs and personalized strategies.
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