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Pulse Afatinib for ERBB2 Exon 20 Insertion–Mutated Lung Adenocarcinomas
Daniel B. Costa, MD, PhD, Susan E. Jorge, PhD, Jason P. Moran, MD, Jason A. Freed, MD, Jessica A. Zerillo, MD, Mark S. Huberman, MD, Susumu S. Kobayashi, MD, PhD Journal of Thoracic Oncology Volume 11, Issue 6, Pages (June 2016) DOI: /j.jtho Copyright © 2016 International Association for the Study of Lung Cancer Terms and Conditions
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Figure 1 Response to erb-b2 receptor tyrosine kinase 2 (ERBB2) tyrosine kinase inhibitors (TKIs) in epidermal growth factor receptor gene (EGFR)- and erb-b2 receptor tyrosine kinase 2 gene (ERBB2)-mutated cell lines. (A) The 50% inhibitory concentration (IC50) of erlotinib using nanomolar (nM) concentrations. (B) IC50 of afatinib using nM concentrations. Cell lines used and genotype are indicated in the figure. The expected median trough plasma concentration of erlotinib, 150 mg/day (∼2000 nM), and afatinib, 40 mg/day (∼60 nM), are plotted. Journal of Thoracic Oncology , DOI: ( /j.jtho ) Copyright © 2016 International Association for the Study of Lung Cancer Terms and Conditions
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Figure 2 Response to pulse afatinib. (A) Waterfall plot of the maximum response to afatinib, 280 mg once weekly. Progressive disease (PD), stable disease (SD), and partial response (PR) are indicated in different colors. (B) Swimmer plot of the duration of response, duration of use of afatinib, and sites of PD in each patient. Post-PD afatinib is shown, when applicable. (C) Computed tomography example of prolonged period of disease control in the patient whose lung adenocarcinoma harbored an ERBB2-V747_G748insGSP mutation. Shown are preafatinib and month 8 of pulse afatinib representative computed tomography scan cuts. The red arrows highlight a pleural-based lesion. ERBB2, erb-b2 receptor tyrosine kinase 2 gene. Journal of Thoracic Oncology , DOI: ( /j.jtho ) Copyright © 2016 International Association for the Study of Lung Cancer Terms and Conditions
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