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Updated: Feb 13, 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
Afatinib in advanced NSCLC: a profile of its use
Emma D Deeks1, Gillian M Keating1
1Springer, Private Bag 65901, Mairangi Bay, 0754 Auckland, New Zealand.
Abstract:
Afatinib [Giotrif® (EU); Gilotrif® (USA)] is an orally administered, irreversible inhibitor of the ErbB family of tyrosine kinases that provides an important first-line treatment option for advanced non-small cell lung cancer (NSCLC) with activating epidermal growth factor receptor (EGFR) mutations (i.e. EGFRactMUT+), and an additional treatment option for squamous NSCLC that has progressed following first-line platinum-based chemotherapy. Relative to gefitinib in the first-line treatment of EGFRactMUT+ advanced lung adenocarcinoma, afatinib prolonged progression-free survival (PFS) and time to treatment failure (TTF), but not overall survival (OS). Afatinib also prolonged PFS, but not OS, versus cisplatin-based chemotherapy in this setting; however, afatinib improved OS versus chemotherapy in the subgroup of patients with deletions in exon 19. As a second-line treatment for advanced squamous NSCLC, afatinib prolonged PFS and OS compared with erlotinib, regardless of EGFR mutation status. Afatinib had a predictable and manageable tolerability profile.
Insights
Afatinib is an effective treatment for advanced non-small cell lung cancer (NSCLC) with EGFR mutations, improving progression-free survival. It also benefits squamous NSCLC patients progressing after chemotherapy.
Area of Science:
- Oncology
- Pharmacology
- Medical Oncology
Background:
- Afatinib is an irreversible ErbB family tyrosine kinase inhibitor.
- It is approved for advanced non-small cell lung cancer (NSCLC) with specific epidermal growth factor receptor (EGFR) mutations and for squamous NSCLC post-chemotherapy.
Purpose of the Study:
- To evaluate afatinib's efficacy and safety in advanced NSCLC.
- Compare afatinib with gefitinib and chemotherapy in the first-line setting for EGFR-mutated NSCLC.
- Assess afatinib versus erlotinib in the second-line setting for advanced squamous NSCLC.
Main Methods:
- Clinical trials comparing afatinib to gefitinib and platinum-based chemotherapy.
- Second-line treatment comparison of afatinib versus erlotinib.
- Analysis of progression-free survival (PFS), time to treatment failure (TTF), and overall survival (OS).
Main Results:
- Afatinib demonstrated prolonged PFS and TTF compared to gefitinib in first-line EGFR-mutated NSCLC, without improving overall survival (OS).
- In the first-line setting, afatinib improved PFS versus chemotherapy, with a notable OS benefit in patients with exon 19 deletions.
- As second-line therapy for squamous NSCLC, afatinib showed improved PFS and OS compared to erlotinib, irrespective of EGFR mutation status.
Conclusions:
- Afatinib is a valuable first-line option for EGFR-mutated NSCLC and an effective second-line treatment for advanced squamous NSCLC.
- Afatinib offers manageable tolerability and demonstrates clinical benefits in specific NSCLC patient populations.
- The drug's efficacy varies depending on the NSCLC subtype, mutation status, and treatment line.
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