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Recent Advances in Boosting EGFR Tyrosine Kinase Inhibitors-Based Cancer Therapy
Qingqing Pan1, Yao Lu2, Li Xie1
1School of Preclinical Medicine, Chengdu University, Chengdu 610106, China.
Abstract:
Epidermal growth factor receptor (EGFR) plays a key role in signal transduction pathways associated with cell proliferation, growth, and survival. Its overexpression and aberrant activation in malignancy correlate with poor prognosis and short survival. Targeting inhibition of EGFR by small-molecular tyrosine kinase inhibitors (TKIs) is emerging as an important treatment model besides of chemotherapy, greatly reshaping the landscape of cancer therapy. However, they are still challenged by the off-targeted toxicity, relatively limited cancer types, and drug resistance after long-term therapy. In this review, we summarize the recent progress of oral, pulmonary, and injectable drug delivery systems for enhanced and targeting TKI delivery to tumors and reduced side effects. Importantly, EGFR-TKI-based combination therapies not only greatly broaden the applicable cancer types of EGFR-TKI but also significantly improve the anticancer effect. The mechanisms of TKI resistance are summarized, and current strategies to overcome TKI resistance as well as the application of TKI in reversing chemotherapy resistance are discussed. Finally, we provide a perspective on the future research of EGFR-TKI-based cancer therapy.
Insights
Targeting epidermal growth factor receptor (EGFR) with tyrosine kinase inhibitors (TKIs) offers new cancer treatments. This review covers advanced drug delivery systems and combination therapies to improve efficacy and overcome resistance.
Area of Science:
- Oncology
- Pharmacology
- Drug Delivery Systems
Background:
- Epidermal growth factor receptor (EGFR) is crucial for cell growth; its overexpression drives malignancy, correlating with poor prognosis.
- Small-molecule tyrosine kinase inhibitors (TKIs) targeting EGFR are a key cancer therapy, but face challenges like toxicity and drug resistance.
Purpose of the Study:
- To review advancements in drug delivery systems for enhanced and targeted delivery of EGFR-TKIs.
- To explore combination therapies involving EGFR-TKIs for broader applications and improved outcomes.
- To summarize mechanisms of TKI resistance and strategies to overcome it, including reversing chemotherapy resistance.
Main Methods:
- Review of recent literature on oral, pulmonary, and injectable drug delivery systems for EGFR-TKIs.
- Analysis of studies on EGFR-TKI combination therapies in various cancer types.
- Summary of research on mechanisms and strategies related to TKI resistance.
Main Results:
- Novel drug delivery systems show promise for targeted TKI delivery, reducing side effects.
- EGFR-TKI combination therapies expand treatment applicability and enhance anticancer effects.
- Understanding TKI resistance mechanisms is crucial for developing effective overcoming strategies.
Conclusions:
- Advanced drug delivery and combination therapies represent significant progress in EGFR-TKI cancer treatment.
- Strategies to overcome TKI resistance are vital for long-term therapeutic success.
- Future research should focus on optimizing EGFR-TKI-based therapies for improved patient outcomes.
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