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Tyrosine kinase inhibitors in breast cancer (Review)
George Iancu1,2, Dragos Serban3,4, Cristinel Dumitru Badiu3,5
1Department of Obstetrics and Gynecology, Faculty of Medicine, 'Carol Davila' University of Medicine and Pharmacy, 020021 Bucharest, Romania.
Abstract:
Anti-epidermal growth factor receptor (EGFR)-targeted therapy has been intensely researched in the last years, motivated by the favorable results obtained with monoclonal antibodies in HER2-enriched breast cancer (BC) patients. Most researched alternatives of anti-EGFR agents were tyrosine kinase inhibitors (TKIs) and monoclonal antibodies. However, excluding monoclonal antibodies trastuzumab and pertuzumab, the remaining anti-EGFR molecules have exhibited disappointing results, due to the lack of specificity and frequent adverse side effects. TKIs have several advantages, including reduced cardiotoxicity, oral administration and favorable penetration of blood-brain barrier for brain metastatic BC. Lapatinib and neratinib and recently pyrotinib (approved only in China) are the only TKIs from dozens of molecules researched over the years that were approved to be used in clinical practice with limited indications, in a subset of BC patients, single or in combination with other chemotherapy or hormonal therapeutic agents. Improved identification of BC subtypes and improved characterization of aggressive forms (triple negative BC or inflammatory BC) should lead to advancements in shaping of targeted agents to improve the outcome of patients.
Insights
Targeted therapies against epidermal growth factor receptor (EGFR) show promise for breast cancer (BC). While some tyrosine kinase inhibitors (TKIs) are approved, further research into BC subtypes is needed for better patient outcomes.
Area of Science:
- Oncology
- Pharmacology
Background:
- Epidermal growth factor receptor (EGFR)-targeted therapy is a key area of breast cancer (BC) research.
- Monoclonal antibodies have shown success in HER2-enriched BC, prompting investigation into other anti-EGFR agents like tyrosine kinase inhibitors (TKIs).
Purpose of the Study:
- To review the development and clinical application of anti-EGFR agents, particularly TKIs, in breast cancer treatment.
- To highlight the challenges and future directions for improving targeted therapies in BC.
Main Methods:
- Literature review of anti-EGFR therapies, including monoclonal antibodies and TKIs.
- Analysis of clinical outcomes and limitations of approved anti-EGFR agents.
Main Results:
- Most anti-EGFR agents, excluding trastuzumab and pertuzumab, have yielded disappointing results due to specificity issues and side effects.
- Few TKIs (lapatinib, neratinib, pyrotinib) are approved for limited BC indications, offering advantages like oral administration and potential for brain metastasis treatment.
- Significant challenges remain in optimizing anti-EGFR therapy efficacy and patient selection.
Conclusions:
- Further research into BC subtypes, especially aggressive forms like triple-negative and inflammatory BC, is crucial.
- Advancements in identifying BC subtypes will guide the development of more effective targeted agents to improve patient outcomes.
