Icotinib - CAS 610798-31-7
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Not Intended for Therapeutic Use. For research use only.
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Icotinib Hydrochloride (BPI-2009H), or Icotinib, is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI).
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1.Icotinib in Patients with Pretreated Advanced Esophageal Squamous Cell Carcinoma with EGFR Overexpression or EGFR Gene Amplification: A Single-Arm, Multicenter Phase 2 Study.
Huang J1, Fan Q2, Lu P3, Ying J4, Ma C5, Liu W6, Liu Y7, Tan F8, Sun Y9. J Thorac Oncol. 2016 Mar 12. pii: S1556-0864(16)00444-5. doi: 10.1016/j.jtho.2016.02.020. [Epub ahead of print]
INTRODUCTION: Epidermal growth factor receptor (EGFR) has been reported to be overexpressed and amplified in a high percentage of patients with esophageal squamous cell carcinoma (ESCC). The activity of icotinib, an EGFR tyrosine kinase inhibitor, was assessed in previously treated ESCC with EGFR overexpression or amplification.
2.Trial-Based Cost-Utility Analysis of Icotinib versus Gefitinib as Second-Line Therapy for Advanced Non-Small Cell Lung Cancer in China.
Zhang C1,2, Zhang H3, Shi J3, Wang D3, Zhang X4, Yang J4, Zhai Q4, Ma A1. PLoS One. 2016 Mar 25;11(3):e0151846. doi: 10.1371/journal.pone.0151846. eCollection 2016.
BACKGROUND: Our objective is to compare the cost-utility of icotinib and gefitinib for the second-line treatment of advanced non-small cell lung cancer (NSCLC) from the perspective of the Chinese healthcare system.
3.Predictive value of EGFR overexpression and gene amplification on icotinib efficacy in patients with advanced esophageal squamous cell carcinoma.
Wang X1, Niu H2, Fan Q3, Lu P4, Ma C5, Liu W6, Liu Y7, Li W4, Hu S1, Ling Y8, Guo L8, Ying J8, Huang J1. Oncotarget. 2016 Mar 22. doi: 10.18632/oncotarget.8271. [Epub ahead of print]
This study aimed to search for a molecular marker for targeted epithelial growth factor receptor (EGFR) inhibitor Icotinib by analyzing protein expression and amplification of EGFR proto-oncogene in esophageal squamous cell carcinoma (ESCC) patients.Immunohistochemistry and fluorescence in situ hybridization (FISH) was used to assess EGFR expression and gene amplification status in 193 patients with ESCC. We also examined the association between EGFR overexpression and the efficacy of a novel EGFR TKI, icotinib, in 62 ESCC patients.Of the 193 patients, 95 (49.2%) patients showed EGFR overexpression (3+), and 47(24.4%) patients harbored EGFR FISH positivity. EGFR overexpression was significantly correlated with clinical stage and lymph node metastasis (p<0.05). In addition, EGFR overexpression was significantly correlated with EGFR FISH positivity (p<0.001). Among the 62 patients who received icotinib, the response rate was 17.6% for patients with high EGFR-expressing tumors, which was markedly higher than the rate (0%) for patients with low to moderate EGFR-expressing tumors (p=0.
4.[Clinical Analysis of Icotinib on Beneficiary of 
Advanced Non-small Cell Lung Cancer with EGFR Common Mutation].
Jiang X1, Wang W1, Zhang Y1. Zhongguo Fei Ai Za Zhi. 2016 Apr 20;19(4):200-6. doi: 10.3779/j.issn.1009-3419.2016.04.04.
in English, Chinese背景与目的 靶向治疗已经成为晚期非小细胞肺癌(non-small cell lung cancer, NSCLC)治疗中不可或缺的重要手段,表皮生长因子受体(epithelial growth factor receptor, EGFR)的酪氨酸激酶抑制剂(tyrosine kinase inhibitor, TKI)可显著延长晚期携带EGFR基因突变肺癌患者生存期。埃克替尼是我国第一个拥有自主知识产权的EGFR-TKI。本研究旨在探讨埃克替尼治疗EGFR敏感突变的晚期NSCLC获益患者的临床特点,对获益患者[无进展生存时间(progression-free survival, PFS)≥6个月]进行回顾性资料收集并分析相关影响因素。方法 收集2011年9月1日-2015年9月30日浙江省肿瘤医院经埃克替尼片治疗的231例EGFR敏感突变的晚期NSCLC获益患者的生存情况。结果 经埃克替尼治疗后,一线治疗组1年获益率达67.9%,二线及以上组为53.6%,具有统计学意义(P=0.027);一线治疗组2年获益率对比二线及以上组亦有统计学差异(18.7%和9.3%,P=0.047)。一线患者和二线及以上患者的中位PFS分别为16.7个月和12.4个月,且差异具有统计学意义(P=0.006)。其中有无脑转移(P=0.010)、埃克替尼治疗时机(P=0.001)、美国东部肿瘤协作组(Eastern Cooperative Oncology Group, ECOG)评分(P=0.001)为影响预后的主要因素。主要不良反应为皮疹51例(22.1%),腹泻27例(11.7%)。结论 埃克替尼是EGFR基因敏感突变的晚期NSCLC患者有效的治疗方案,其优势人群除无脑转移者及ECOG评分好的患者外,一线治疗患者疗效明显优于二线及以上者。敏感突变患者采用埃克替尼可得到较好的临床获益,并具有较好的耐受性。.
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CAS 610798-31-7 Icotinib

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