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Updated: Apr 28, 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 (BIBW 2992)]
N Prim1, M Fore1, B Mennecier1
1Service de pneumologie, pôle de pathologie thoracique, nouvel hôpital civil, hôpitaux universitaires de Strasbourg, 1, porte de l'Hôpital, 67091 Strasbourg cedex, France.
Abstract:
Afatinib (BIBW 2992) is an irreversible multi-target HER receptor tyrosine kinase inhibitor developed in patients with advanced solid tumours. Several phase I studies were conducted in patients with non-small cell lung cancer (NSCLC), as a single agent or in combination. In further phase II or III studies, patients were selected based on the duration of response to first generation EGFR-TKI in previous line (supposed to have greater chance to have an activating EGFR mutation) or based directly on the EGFR activating mutation status. Here, we report and comment the main results of these studies in lung cancer patients. This drug has been approved by the Food and Drug Administration in June 2013 for the first-line treatment of patients with metastatic NSCLC whose tumours have EGFR mutation. In Europe, it has been approved in September 2013 in the same indication.
Insights
Afatinib, an irreversible HER receptor tyrosine kinase inhibitor, shows promise for advanced solid tumors, particularly metastatic non-small cell lung cancer (NSCLC) with EGFR mutations. It received FDA and European approval in 2013 for first-line treatment.
Area of Science:
- Oncology
- Pharmacology
Background:
- Afatinib is an irreversible multi-target HER receptor tyrosine kinase inhibitor.
- Investigated for advanced solid tumors, including non-small cell lung cancer (NSCLC).
Purpose of the Study:
- To report and comment on the main results of clinical studies involving afatinib in lung cancer patients.
- Evaluate afatinib's efficacy in advanced solid tumors, particularly NSCLC.
Main Methods:
- Phase I, II, and III clinical studies were conducted.
- Patient selection based on prior EGFR-TKI response or EGFR activating mutation status.
- Afatinib administered as a single agent or in combination therapies.
Main Results:
- Afatinib demonstrated efficacy in patients with advanced solid tumors.
- Specific focus on metastatic NSCLC patients with EGFR mutations.
- Received FDA approval in June 2013 and European approval in September 2013 for first-line treatment of metastatic NSCLC with EGFR mutations.
Conclusions:
- Afatinib is an approved targeted therapy for first-line treatment of metastatic NSCLC with EGFR mutations.
- The drug's development involved extensive clinical trials to establish its efficacy and safety profile.
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