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Updated: Sep 25, 2026

Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
Published on: June 26, 2019
[Epidermal growth factor inhibitors]
C Delbaldo1, S Faivre, E Raymond
1Département de médecine, institut Gustave-Roussy, 39, rue Camille-Desmoulins, 94805 cedex, Villejuif, France.
Purpose:
Tyrosine kinases are implicated in the normal cellular proliferation and in malignant transformation. Among the tyrosine kinase receptors, one of best described is the Epidermal Growth Factor Receptor (EGFR), which is widely expressed in particular in epithelial cells and in many human carcinomas.
Current Knowledge And Key Points:
Compounds have been developed that target either the extracellular ligand-binding region of EGFR (Cetuximab) or the intracellular tyrosine kinase ATP-binding (Iressa), Tarceva. Phase I studies showed that these molecules have a favorable pharmacokinetic and pharmacodynamic profile, with excellent tolerance and easy administration. Phase II and III studies are currently testing their efficacy.
Future Prospects And Projects:
Preliminary results show interesting activity in different tumors, alone or in combination with either chemotherapy or radiotherapy. If these results are confirmed in larger trials including a high number of patients, these agents might be very useful in combination with chemotherapy, radiotherapy or other biological targeting agents such as cellular cycle inhibitors or antiangiogenics.
Insights
Targeting Epidermal Growth Factor Receptor (EGFR) with new drugs shows promising results in cancer treatment. These agents, including Cetuximab, Iressa, and Tarceva, are well-tolerated and may enhance chemotherapy and radiotherapy efficacy.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Tyrosine kinases play a crucial role in cell proliferation and cancer development.
- Epidermal Growth Factor Receptor (EGFR) is a key tyrosine kinase receptor implicated in various human carcinomas.
- Targeted therapies are being developed to inhibit EGFR signaling pathways.
Purpose of the Study:
- To review the role of tyrosine kinases and EGFR in cancer.
- To discuss the development and preliminary findings of EGFR-targeting agents.
- To evaluate the potential of these agents in cancer treatment strategies.
Main Methods:
- Review of existing literature on EGFR inhibitors.
- Analysis of Phase I, II, and III clinical trial data.
- Pharmacokinetic and pharmacodynamic profiling of targeted agents.
Main Results:
- EGFR inhibitors (Cetuximab, Iressa, Tarceva) demonstrate favorable safety and tolerability.
- Early studies indicate promising anti-tumor activity for these agents.
- Combination therapies with chemotherapy or radiotherapy are under investigation.
Conclusions:
- EGFR-targeted therapies show potential as effective cancer treatments.
- Further large-scale trials are needed to confirm efficacy.
- These agents may be valuable additions to multimodal cancer therapy, including combination with other targeted agents.
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