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EGFR-targeted tyrosine kinase inhibitors: advancements in cancer therapy
Shaheen Ali1,2, Anam Ilyas2, Shagufi Nazar2
1Department of Molecular Medicine, School of Interdisciplinary Sciences and Technology, Jamia Hamdard, New Delhi, 110062, India.
Abstract:
Cancer treatment has changed significantly with the advent of EGFR-targeted TK inhibitors (TKIs), especially for non-small cell lung cancer (NSCLC). Despite their effectiveness, problems including acquired resistance, particularly the T790M mutation, and non-specific toxicity still exist. Recent developments in drug delivery, combination therapy, and knowledge of resistance mechanisms are addressing these issues. The efficacy of EGFR-targeted therapy has been demonstrated in a wide range of cancers, including head and neck and colorectal cancers. Genomic profiling informs precision medicine, which improves treatment approaches. Targeted cancer therapies, including kinase inhibitors and monoclonal antibodies, block specific signaling pathways essential for tumor growth, offering a more precise alternative to traditional chemotherapy. Moreover, nanotechnology enhances drug delivery, reduces toxicity, and overcomes resistance through advanced nanoparticles like polymeric micelles, PLGA, and chitosan, improving solubility, bioavailability, and sustained EGFR TKI release. This review discusses EGFR's significance in cancer therapy, the evolution of EGFR-targeted TKIs, resistance challenges, and advancements in nanotechnology-based drug delivery. We explore how polymeric and inorganic nanoparticles improve pharmacokinetics and targeted delivery, offering promising solutions to overcome resistance and enhance the therapeutic potential of EGFR-targeted therapies in personalized oncology.
Insights
Epidermal Growth Factor Receptor (EGFR)-targeted therapies, including tyrosine kinase inhibitors (TKIs), are revolutionizing cancer treatment. Nanotechnology offers solutions to overcome resistance and reduce toxicity in EGFR-targeted therapies.
Area of Science:
- Oncology
- Pharmacology
- Nanotechnology
Background:
- Epidermal Growth Factor Receptor (EGFR) targeted therapies, particularly tyrosine kinase inhibitors (TKIs), have transformed non-small cell lung cancer (NSCLC) treatment.
- Acquired resistance, notably the T790M mutation, and off-target toxicity remain significant challenges in EGFR-targeted therapy.
- EGFR's role extends beyond NSCLC, with demonstrated efficacy in head and neck and colorectal cancers.
Purpose of the Study:
- To review the significance of EGFR in cancer therapy and the evolution of EGFR-targeted TKIs.
- To discuss challenges related to resistance mechanisms and toxicity associated with EGFR-targeted therapies.
- To explore advancements in nanotechnology-based drug delivery systems for enhancing EGFR-targeted therapies.
Main Methods:
- Review of current literature on EGFR-targeted therapies, resistance mechanisms, and nanotechnology applications in drug delivery.
- Analysis of how genomic profiling informs precision medicine approaches in oncology.
- Exploration of nanoparticle-based drug delivery systems (polymeric micelles, PLGA, chitosan) for improving EGFR TKI pharmacokinetics and overcoming resistance.
Main Results:
- EGFR-targeted TKIs offer a more precise alternative to traditional chemotherapy by blocking specific tumor growth pathways.
- Nanoparticles enhance drug solubility, bioavailability, and sustained release of EGFR TKIs, thereby reducing toxicity.
- Polymeric and inorganic nanoparticles demonstrate potential in improving pharmacokinetics and targeted delivery, crucial for overcoming resistance.
Conclusions:
- Nanotechnology-based drug delivery presents promising solutions to overcome acquired resistance and reduce toxicity in EGFR-targeted cancer therapies.
- Advancements in drug delivery, combination therapy, and understanding resistance mechanisms are crucial for improving therapeutic outcomes.
- Personalized oncology benefits from integrating genomic profiling with advanced targeted therapies and novel drug delivery systems.
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