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Updated: Aug 19, 2025

Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure
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Understanding and Targeting the Epigenetic Regulation to Overcome EGFR-TKIs Resistance in Human Cancer

Lan Sun1, Lingyue Gao1, Yingxi Zhao1

  • 1Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, PR China.

Recent Patents on Anti-Cancer Drug Discovery
|December 5, 2022
PubMed
Abstract

Insights

Combining epigenetic drugs with other therapies can overcome resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), improving patient survival in various cancers. Further research is needed on optimal dosing and novel targets.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Cancer development involves genetic and epigenetic dysregulation, with histone modification crucial for gene expression.
  • Epidermal growth factor receptor (EGFR) overexpression promotes cancer, making EGFR-targeted therapies essential.
  • Resistance to EGFR tyrosine kinase inhibitors (EGFR-TKIs) is a significant clinical challenge, limiting treatment efficacy.

Approach:

  • This study explores overcoming EGFR-TKIs resistance through combination therapy.
  • Epigenetic drugs are investigated as a strategy to reverse acquired resistance mechanisms.

Key Points:

  • Epigenetic modifications reversibly alter gene transcription without changing DNA sequence.
  • EGFR-TKIs resistance, often developing within a year, necessitates novel therapeutic strategies.
  • Combination therapy involving epigenetic drugs shows promise in overcoming EGFR-TKIs resistance.

Conclusions:

  • Epigenetic agents offer a promising approach to counteract EGFR-TKIs resistance in human cancers.
  • Future research should focus on identifying new epigenetic targets beyond histone deacetylases (HDACs).
  • Optimizing the dosage and administration of epigenetic combination therapies requires further clinical investigation.
Keywords:
EGFR-TKIsEpigenetic regulationcancerclinical trialscombination therapypatentresistant mechanisms

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