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Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
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Afatinib for the treatment of advanced non-small-cell lung cancer

Carlo Genova1, Erika Rijavec, Giulia Barletta

  • 1UOS Tumori Polmonari, IRCCS AOU San Martino - IST Istituto Nazionale per la Ricerca sul Cancro , L.go Benzi 10, Genova 16132 , Italy carlo.genova1985@gmail.com.

Expert Opinion on Pharmacotherapy
|March 21, 2014
PubMed
Abstract

Insights

Afatinib is an effective first-line treatment for EGFR-mutated non-small cell lung cancer (NSCLC), improving outcomes compared to chemotherapy. Further research is needed to clarify its role in acquired resistance to EGFR tyrosine kinase inhibitors (TKIs).

Area of Science:

  • Oncology
  • Pharmacology
  • Clinical Medicine

Background:

  • Epidermal Growth Factor Receptor (EGFR) tyrosine kinase inhibitors (TKIs) are key in treating EGFR-mutated Non-Small Cell Lung Cancer (NSCLC).
  • Afatinib, an irreversible ErbB family blocker, targets EGFR, HER2, and HER4, and ErbB3 transphosphorylation.
  • Afatinib is approved for first-line treatment of EGFR-mutated NSCLC in the US and for TKI-naive patients in Europe and Japan.

Purpose of the Study:

  • To review the pharmacology and clinical activity of afatinib in NSCLC.
  • To evaluate afatinib's efficacy and safety in various treatment settings.
  • To identify areas where further clinical data is required.

Main Methods:

  • Literature review of pharmacology and clinical activity of afatinib.
  • Analysis of clinical trials, including LUX-Lung 3 and LUX-Lung 6.
  • Assessment of efficacy, safety, and quality of life outcomes.

Main Results:

  • Afatinib demonstrated superior outcomes (response rate, progression-free survival, quality of life) compared to chemotherapy in trials like LUX-Lung 3 and LUX-Lung 6.
  • The primary toxicities associated with afatinib include gastrointestinal and skin-related adverse events.
  • Afatinib shows efficacy as a first-line treatment for common EGFR mutations in NSCLC.

Conclusions:

  • Afatinib is highly effective as a first-line therapy for EGFR-mutated NSCLC.
  • Afatinib exhibits some activity in NSCLC with acquired resistance to EGFR TKIs, but its efficacy post-erlotinib or gefitinib failure requires further clarification.
  • Direct comparative clinical data on the activity and tolerability of different EGFR inhibitors are still needed.

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