[6]Lim SM, Kim HR, Cho EK, et al. Targeted sequencing identifies genetic alterations that confer primary resistance to EGFR tyrosine kinase inhibitor (Korean Lung Cancer Consortium). Oncotarget. 2016 Jun 14;7(24):36311-36320. DOI: 10.18632/oncotarget.8904 [7]Jin Y, Shi X, Zhao J, et ...
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表皮生长因子受体酪氨酸激酶抑制剂(epithelial growth factor receptor-tyrosine kinase inhibitors, EGFR-TKIs)给局部晚期或转移EGFR突变阳性的非小细胞肺癌(non-small cell lung carcinoma, NSCLC)患者带来生存获益。然而,NSCLC患者通常同时服用EGFR-TKIs与其他药物,尤其...
2023年8月3日,耶鲁癌症中心Katerina A. Politi团队与丹娜-法伯癌症研究所和哈佛医学院小儿肿瘤科Cigall Kadoch团队合作,在Cancer Cell期刊以长文形式发表了文章Mammalian SWI/SNF chromatin remodeling complexes promote tyrosine kinase inh...
ATP竞争性EGFR酪氨酸激酶抑制剂的成功开发(Tyrosine kinase inhibitors, TKIs),对治疗EGFR突变的NSCLC产生了巨大的影响。但获得性耐药的发生限制了EGFR TKIs的长期疗效。其中,C797S 突变及其与其他多种突变的组合是目前 EGFR-TKI 面临的耐药新难题,也是目前第三代EGFR抑制剂的主要耐药机制,开发高亲和力的可逆性抑制剂或...
1. Yang Z, Yang N, Ou Q, et al. Investigating Novel Resistance Mechanisms to Third-Generation EGFR Tyrosine Kinase Inhibitor Osimertinib in Non-Small Cell Lung Cancer Patients. Clin Cancer Res. 2018 Jul 1;24(13):3097-3107. 2. Le X, Puri S, Negrao MV, et al. Landscape of EGFR-Depen...
[4] Lu S, et al. Sintilimab plus bevacizumab biosimilar IBI305 and chemotherapy for patients with EGFR-mutated non-squamous non-small-cell lung cancer who progressed on EGFR tyrosine-kinase inhibitor therapy (ORIENT-31): first interim results from a randomised, double-blind, multicentre, phase...
[3]Yi-Long Wu, Ying Cheng, Jianying Zhou, et al. Tepotinib plus gefitinib in patients with EGFR-mutant non-small-cell lung cancer with MET overexpression or MET amplification and acquired resistance to previous EGFR inhibitor (INSIGHT study): anopen-label, phase 1b/2, multicentre, randomised...
其中NSCLC(non-small cell lung cancer,非小细胞肺癌)占所有肺癌比例约80%,表皮生长因子受体-酪氨酸激酶抑制剂(epidermal growth factor receptor-tyrosine kinase inhibitors, EGFR-TKIs)对于EGFR阳性突变的非小细胞肺癌患者具有良好的耐受性和抗肿瘤活性[1],并得到了广泛的临床应用。然而,EGFR-TKIs在治疗过程中常发生...
从上世纪九十年代开始,针对EGFR这一个抗肿瘤靶点,不同研究者开展了不同的药物开发策略。从已上市产品来看,主要有抑制细胞外配体-受体结合的EGFR单抗类药物,和抑制细胞内ATP-TK结合的TKI(tyrosine kinase inhibitor)小分子化学药物。 由于单抗类药物和TKI类药物的开发策略、适用人群、检测方法、伴随诊断解决方案不同,下...