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Brain metastasis in non-small cell lung cancer (NSCLC) patients with uncommon egfr mutations： a report of seven cases and literature review

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Cancer Biology & Medicine 2017年第4期14卷 418-425页

作者： Puchun Er Tian Zhang Jing Wang Qingsong Pang Ping Wang Department of Radiotherapy Tianjin Medical University Cancer Institute and Hospital National Clinical Research Center for Cancer Key Laboratory of Cancer Prevention and Therapy Tianjin Tianjin's Clinical Research Center for Cancer Tianjin 300060 China

Brain metastasis(BM)arising from non-small cell lung cancer(NSCLC)with rare epidermal growth factor receptor(egfr)mutations is quite *** prognosis and therapeutic effects of BM remain *** the best of our knowledge,this is the first report to make a separate analysis of BM from NSCLC patients with original uncommon egfr *** retrospectively reviewed 7 cases of BM arising from 42 cases of uncommon egfr mutated lung cancer in Tianjin Medical University Cancer Institute and *** also performed a literature review to assess therapeutic features and outcomes.

关键词： Brain metastasis NSCLC uncommon egfr mutations egfr-TKIs brain radiotherapy chemotherapy

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Antitumor activity of aumolertinib, a third-generation egfr tyrosine kinase inhibitor, in non-small-cell lung cancer harboring uncommon egfr mutations

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Acta Pharmaceutica Sinica B 2023年第6期13卷 2613-2627页

作者： Chen Shi Cong Zhang Zhiwen Fu Jinmei Liu Yuanfeng Zhou Bao Cheng Cong Wang Shijun Li Yu Zhang Department of Pharmacy Union HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430022China Hubei Province Clinical Research Center for Precision Medicine for Critical Illness Wuhan 430022China Department of Preclinical Translational Science Shanghai Hansoh Biomedical Co.Ltd.Shanghai 201203China Department of Chemistry Shanghai Hansoh Biomedical Co.Ltd.Shanghai 201203China

uncommon epidermal growth factor receptor(egfr) mutations account for 10% 20% of all egfr mutations in non-small-cell lung cancer(NSCLC). The uncommon egfr-mutated NSCLC is associated with poor clinical outcomes and generally achieved unsatisfactory effects to the current therapies using standard egfr-tyrosine kinase inhibitors(TKIs), including afatinib and osimertinib. Therefore, it is necessary to develop more novel egfr-TKIs to treat uncommon egfr-mutated *** is a third-generation egfr-TKI approved in China for treating advanced NSCLC with common egfr mutations. However, it remains unclear whether aumolertinib is effective in uncommon egfr-mutated NSCLC. In this work, the in vitro anticancer activity of aumolertinib was investigated in engineered Ba/F3 cells and patient-derived cells bearing diverse uncommon egfr mutations. Aumolertinib was shown to be more potent in inhibiting the viability of various uncommon egfr-mutated cell lines than those with wild-type egfr. And in vivo, aumolertinib could also significantly inhibit tumor growth in two mouse allograft models(V769-D770insASV and L861Q mutations) and a patientderived xenografts model(H773-V774insNPH mutation). Importantly, aumolertinib exerts responses against tumors in advanced NSCLC patients with uncommon egfr mutations. These results suggest that aumolertinib has the potential as a promising therapeutic candidate for the treatment of uncommon egfr-mutated NSCLC.

关键词： Aumolertinib Non-small cell lung cancer Oncology uncommon egfr mutations Exon 20 insertion egfr tyrosine kinase inhibitor Targeted therapy Anti-tumor activity

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