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Epidermal Growth Factor Receptor (EGFR) Inhibitors

Overview

Treatment Response

EGFR Inhibitor Resistance & 2nd Mutations

Testing for EGFR Mutations

Tarceva vs Iressa

Iressa (gefitinib) Information

Tarceva (erlotinib) Information

Erbitux (cetuximab) Information

Overview

EGFR Inhibitors: What Have We Learned From the Treatment of Lung Cancer? (Medscape)
Aimed at physicians, this Medscape article (reprinted from Nat Clin Pract Oncol v.2 no.11 2005: 554-561) reviews experience with EGFR inhibitors in lung cancer. Topics covered include: mutations associated with responsiveness, additional markers to predict response, acquired resistance, selection of patients for treatment with EGFR inhibitors. Registration required for free access to Medscape. [11/05]

Targeting Targeted Therapy (New England Journal of Medicine)
by Mark R. Green, MD
v.350, no.21 NEJM (May 20, 2004)
Editorial accompanying an article by Thomas J. Lynch, MD, et al: "Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of NSCLC to Gefitinib." Explores the issues raised by this research for understanding how targeted therapy can be optimized. Aimed at physicians. [5/04]

Breathing New Life into Lung Cancer Treatment (curetoday.com)
Clear explanation of how epidermal growth factor receptor (EGFR) inhibitors work against lung cancer Includes discussion of Iressa, Tarceva and Erbitux. Aimed at patients. [4/02]

MSKCC Advances Lung Cancer Research: Iressa & Tarceva (Memorial Sloan-Kettering Cancer Center)
Relates the role of MSK researchers in the discovery and development surrounding two targeted therapies for lung cancer: Iressa (gefitinib) & Tarceva (erlotinib) and the challenges that lie ahead. Discusses ongoing research into the genetic mutations associated with treatment response and drug resistance.



Treatment Response

Activating Mutations in Epidermal Growth Factor Receptor Underlying Responsiveness of NSCLC to Gefitinib (New England Journal of Medicine)
by Thomas J. Lynch, MD et al.
v.350, no.21 NEJM (May 20, 2004)
Reports the results of a study that found a subgroup of patients with NSCLC who have specific mutations in the EGFR gene, which correlate with clinical responsiveness to the tyrosine kinase inhibitor gefitinib. Screening for such mutations in lung cancer may identify patients who will respond to gefitinib. Full text available as PDF file. See also the accompanying editorial by Mark R. Green, MD: "Targeting Targeted Therapy."] [5/04]

EGFR Mutations & Gefitinib (Iressa & Tarceva) - Recent MEDLINE Abstracts (PubMed)

BAC & EGFR Inhibitors (Iressa & Tarceva) - Recent MEDLINE Abstracts (PubMed)

Asian Ethnicity & EGFR Inhibitors (Iressa & Tarceva) - Recent MEDLINE Abstracts (PubMed)

Never Smokers & EGFR Inhibitors (Iressa & Tarceva) - Recent MEDLINE Abstracts (PubMed)



EGFR Inhibitor Resistance & 2nd Mutations

New Class of Drugs May Treat Lung Tumors Resistant to Iressa and Tarceva (Massachusetts General Hospital)
Discusses the discovery of a new class of drugs that block the epidermal growth factor receptor (EGFR) on lung cancer cells and may get around the problem of resistance to targeted therapies, such as Iressa and Tarceva. Summarizes a report to appear in the Proceedings of the National Academy of Science that describes the mechanism by which "irreversible EGFR inhibitors" apparently avoid resistance and may offer patients longer term remission. [5/05]

EGFR Mutation and Resistance of NSCLC to Gefitinib (Iressa) (PubMed)
Reports a case in the February 24 issue of the New England Journal of Medicine of a patient with EGFR-mutant, gefitinib-responsive, advanced NSCLC who had a relapse after two years of complete remission during treatment with gefitinib (Iressa). The DNA sequence of the EGFR in the patient's tumor biopsy specimen at relapse revealed the presence of a second point mutation. Structural modeling and biochemical studies showed that this second mutation let to gefitinib (Iressa) resistance. [2/05]

Overcoming Acquired Resistance to Iressa/Tarceva with Inhibitors of a Different Class (PubMed)
Study published in the August 2005 issue of Cell Cycle reports findings demonstrating that a distinct class of EGFR inhibitors may overcome some mechanisms of secondary drug resistance in these tumors and may therefore be useful in treating lung cancer patients who initially responded to Iressa or Tarceva and eventually relapsed. [8/05]

Iressa (gefitinib) Resistance & 2nd Mutations - Recent MEDLINE Abstracts (PubMed)


Testing for EGFR Mutations

Molecular Test Helps Guide Treatment for Lung Cancer (Partners Healthcare)
Provides details on the EGFR Kinase Domain Sequencing Test that detects mutations in a critical part of the gene called epidermal growth factor receptor (EGFR). The gene mutation is present in a subset of NSCLC, most commonly patients with adenocarcinoma and bronchioloalveolar carcinomas arising in nonsmokers. When the mutation is present, it is associated with a response to the anti-cancer drug Iressa (gefitinib). Discusses the two studies leading to this finding and provides a link for further information on accessing the test. [9/04] Click here for further information on the EGFR mutation test being developed for commercial use by Genzyme (in conjunction with MGH and DFCI).



Tarceva vs Iressa

The Current Situation: Erlotinib (Tarceva) vs Gefitinib (Iressa) (The Oncologist)
v.10, no.7 The Oncologist (August 2005): 467-470
Aimed at physicians, this article examines the research to date involving erlotinib (Tarceva) and gefitinib (Iressa). Summarizes the results of trials, discusses pertinent issues (effect of smoking status, importance of dose, egfr expression, egfr mutation status) and identifies areas for further study. [8/05]




 

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Last modified: 18-Feb-2009
Karen Parles, MLS Editor