Related Experiment Video
Updated: Aug 1, 2026

Establishing 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
Clinical implications of the mechanism of epidermal growth factor receptor inhibitors
1Division of Hematology/Oncology, Lombardi Cancer Center, Georgetown University Medical Center, Washington, DC 20007, USA. marshalj@georgetown.edu
Abstract:
Novel therapeutic agents that target the epidermal growth factor receptor (EGFR) constitute an important addition to the therapeutic armamentarium for the treatment of metastatic disease. EGFR-targeted agents currently approved by the U.S. Food and Drug Administration include cetuximab, a monoclonal antibody for the treatment of colorectal cancer; and the small-molecule EGFR tyrosine kinase inhibitor (TKI) erlotinib for the treatment of nonsmall cell lung cancer (NSCLC) and pancreatic cancer. Approval of the TKI gefitinib for NSCLC recently was withdrawn. Although both classes of anti-EGFR agents target the same receptor, substantial distinctions regarding their mechanism significantly affect dosing requirements, toxicity profiles, and their use as combination agents.
Insights
Novel therapies targeting the epidermal growth factor receptor (EGFR) offer new options for metastatic disease. Different EGFR-targeted agents, like monoclonal antibodies and tyrosine kinase inhibitors, have distinct mechanisms, affecting treatment and toxicity.
Area of Science:
- Oncology
- Pharmacology
Background:
- Novel therapeutic agents targeting the epidermal growth factor receptor (EGFR) are crucial for treating metastatic diseases.
- Approved EGFR-targeted agents include cetuximab (monoclonal antibody) for colorectal cancer and erlotinib (tyrosine kinase inhibitor) for NSCLC and pancreatic cancer.
- Gefitinib, an EGFR tyrosine kinase inhibitor, recently had its U.S. FDA approval withdrawn.
Purpose of the Study:
- To review the current landscape of EGFR-targeted therapies.
- To highlight the distinctions between different classes of anti-EGFR agents.
- To discuss the implications of these distinctions on clinical use.
Main Methods:
- Literature review of FDA-approved EGFR-targeted agents.
- Comparative analysis of monoclonal antibodies and small-molecule tyrosine kinase inhibitors.
- Examination of mechanisms of action, dosing, toxicity, and combination therapy potential.
Main Results:
- Cetuximab and erlotinib are approved EGFR-targeted therapies.
- EGFR-targeted agents, despite targeting the same receptor, possess significant mechanistic differences.
- These differences impact dosing, toxicity profiles, and suitability for combination therapies.
Conclusions:
- EGFR-targeted agents represent a significant advancement in cancer therapy.
- Understanding the mechanistic differences between anti-EGFR agents is critical for optimizing treatment strategies.
- Further research is needed to fully elucidate the clinical implications of these distinctions.
More Related Videos
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
15:05Deciphering the Structural Effects of Activating EGFR Somatic Mutations with Molecular Dynamics Simulation
Published on: May 20, 2020
Related Concept Videos
Mitogens and the Cell Cycle
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Receptor Downregulation in MVBs
The EGFR can initiate signaling pathways that lead to cell proliferation, migration, and differentiation. Overexpression of EGFR stimulates cells to proliferate. Excessive EGFR activation may...
Role of Ephrin-Eph Signalling in Intestinal Stem Cell Renewal
Clinical Applications of Epidermal Stem Cells
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include: