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Alectinib

肿瘤

关键词肿瘤 药物 肺癌

词汇介绍

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解析

Alectinib

释    义   n. 艾乐替尼;阿雷替尼;阿来替尼

例    句   There are currently several ALK inhibitors, including crizotinib, ceritinib, alectinib, brigatinib, and lorlatinib which have been licensed by the US Food and Drug Administration or the European Medicines Agency for the treatment of ALK+ NSCLC patients. 目前有几种ALK抑制剂,包括克唑替尼、色瑞替尼、阿来替尼、布加替尼和劳拉替尼,已经获得美国食品和药物管理局或欧洲药物管理局的许可,用于治疗ALK+非小细胞肺癌患者。

概述

阿来替尼也叫艾乐替尼,Alectinib是一种酪氨酸激酶抑制剂靶向作用于ALK和RET。艾乐替尼能够抑制ALK磷酸化和ALK-介导的下游信号蛋白STAT3和AKT的激活,并且抑制ALK融合、扩增等。降低肿瘤细胞的活力,最终促进肿瘤细胞的凋亡。ALK是一种间变性淋巴瘤激酶,在ALK突变的患者中由于染色体结构发生了改变,导致EML4基因与ALK基因的重排,使肿瘤细胞进展。   2015年12月,美国FDA批准罗氏的艾乐替尼上市,用于克唑替尼耐药

Rapid Acquisition of Alectinib Resistance in ALK-Positive Lung Cancer With High Tumor Mutation Burden复制标题

高肿瘤突变负荷的ALK阳性肺癌中快速获得Alectinib耐药

发表时间:2019-11-05

影响因子:12.5

作者: Go Makimoto

期刊:J Thorac Oncol

NTRODUCTION: The highly selective ALK receptor tyrosine kinase (ALK) inhibitor alectinib is standard therapy for ALK-positive lung cancers; however, some tumors quickly develop resistance. Here, we investigated the mechanism associated with rapid acquisition of resistance using clinical samples.   METHODS: Autopsied samples were obtained from lung, liver, and renal tumors from a 51-year-old male patient with advanced ALK-positive lung cancer who had acquired resistance to alectinib in only 3 months. We established an alectinib-resistant cell line (ABC-14) from pleural effusion and an alectinib/crizotinib-resistant cell line (ABC-17) and patient-derived xenograft (PDX) model from liver tumors. Additionally, we performed next-generation sequencing, direct DNA sequencing, and quantitative real-time reverse transcription polymerase chain reaction.

译文

简介:高选择性ALK受体酪氨酸激酶(ALK)抑制剂阿力克替尼(alctinib)是ALK阳性肺癌的标准治疗药物,但有些肿瘤很快产生耐药性。在这里,我们利用临床样本研究了快速获得耐药性的相关机制。 方法:对一例51岁男性晚期ALK阳性肺癌患者,在3个月内对阿莱克汀产生耐药性,从肺、肝、肾肿瘤中采集尸检标本。我们建立了胸腔积液中阿列克替尼耐药细胞株(ABC-14)和肝癌中阿列克替尼/环唑替尼耐药细胞株(ABC-17)及患者源性异种移植(PDX)模型。此外,我们还进行了下一代测序、直接DNA测序和定量实时逆转录聚合酶链反应。