Related Experiment Video
Updated: May 8, 2026
Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
Published on: December 9, 2015
A Review on EGFR-Tyrosine Kinase Inhibitors and their Resistance Mechanisms
Mohd Javed Naim1, Abdul Samad1
1Pharmacy Department, Tishk International University, Erbil, Iraq.
Background:
An essential component of cell development, proliferation, and survival is the transmembrane receptor known as the epidermal growth factor receptor (EGFR). Dysregulated EGFR signalling is an appealing pathway that has been linked to the genesis and progression of several cancer types. EGFR tyrosine kinase inhibitors (TKIs) are targeted drugs that show promise in the fight against cancer. EGFR tyrosine kinase inhibitors obstruct cancer growth and survival signalling pathways by blocking the receptor's tyrosine kinase domain. Patients with non-small cell lung cancer (NSCLC) that have EGFR mutations have shown increased progression-free survival and overall survival rates when treated with EGFR TKIs as compared to conventional chemotherapy, according to many clinical studies.
Objectives:
This review is aimed to present the journey of EGFR-tyrosine kinase inhibitors, their signalling cascade, and various resistant mechanisms.
Methods:
The literature search was carried out on electronic databases like PubMed, Medline, etc., by employing search keywords, such as EGFR, EGFR inhibitors, cancer, tyrosine kinase, etc., and data on EGFR signaling pathways and the types of potential inhibitors in a hierarchical manner, followed by various resistance mechanisms that have emerged, were collected.
Results:
Drug resistance is still an issue in long-term therapy of patients, even though EGFR TKIs provide substantial therapeutic advantages. Common routes of resistance to EGFR TKIs include acquired resistance mechanisms, which include the development of secondary EGFR mutations and the activation of alternative signalling pathways. To improve the therapeutic effectiveness of EGFR TKIs, future research will center on searching indicators of response and resistance, finding ways to employ these medicines most effectively, and creating new treatment approaches.
Conclusion:
This review provides insight into the use of EGFR kinase inhibitors for treating cancer patients and outlines potential advancements in current therapies to develop more effective molecules.
Insights
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) show promise in cancer treatment, particularly for non-small cell lung cancer. However, drug resistance remains a challenge, necessitating further research into overcoming these mechanisms for improved patient outcomes.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Epidermal growth factor receptor (EGFR) is crucial for cell development and survival.
- Dysregulated EGFR signaling drives various cancer types.
- EGFR tyrosine kinase inhibitors (TKIs) are targeted therapies for cancer treatment.
Purpose of the Study:
- To review the development of EGFR-tyrosine kinase inhibitors.
- To elucidate EGFR signaling pathways.
- To explore mechanisms of resistance to EGFR TKIs.
Main Methods:
- Literature search conducted on electronic databases (PubMed, Medline).
- Keywords used: EGFR, EGFR inhibitors, cancer, tyrosine kinase.
- Data collected on EGFR signaling, inhibitors, and resistance mechanisms.
Main Results:
- EGFR TKIs offer significant therapeutic benefits, especially in EGFR-mutated non-small cell lung cancer.
- Acquired resistance, including secondary EGFR mutations and alternative pathway activation, limits long-term efficacy.
- Future research focuses on identifying response/resistance indicators and developing novel therapeutic strategies.
Conclusions:
- EGFR kinase inhibitors are valuable in cancer therapy.
- Further advancements are needed to enhance therapeutic effectiveness and overcome resistance.
- Development of more potent and effective EGFR-targeted molecules is ongoing.
More Related Videos
09:38Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure
Published on: August 11, 2017
09:38Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
Published on: June 26, 2019
Related Concept Videos
02:38Mitogens and the Cell Cycle
02:57Targeted Cancer Therapies
There are several types of targeted therapies against specific...
02:56Treatment Resistant Cancers
02:53Adaptive Mechanisms in Cancer Cells
Some of the advantages that cancer cells have on normal cells include - enhanced ability to divide without terminally differentiating, induce new blood vessel formation,...
02:56Treatment Resistent Cancers
01:11Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase