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<p>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.</p> Graphical Abstract <p></p>

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EGFR-targeted tyrosine kinase inhibitors: advancements in cancer therapy

  • 期刊论文

  • 发表日期：

    2025年10月27日

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  • Shaheen Ali,
  • Anam Ilyas,
  • Shagufi Nazar,
  • Mukund Jha,
  • Vishal Mathur,
  • Sana Tanweer,
  • Sonam Grover,
  • Ozair Alam

摘要

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.

Graphical Abstract