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Crizotinib

肿瘤

关键词肿瘤 药物 肺癌

词汇介绍

拓展阅读

解析

Crizotinib 

释    义   n. 克唑替尼(药物名称)

例    句   Crizotinib activity in patients with ROS1-translocated tumours was confirmed. 克唑替尼在ROS1易位肿瘤患者中的活性得到证实。

概述

克唑替尼,商品名叫Xalkori,赛可瑞。为粉红色硬胶囊剂,内容物为白色结晶粉末。是辉瑞制药研制的一种口服酪氨酸激酶受体抑制剂,在美国于2011年上市,用于治疗间变性淋巴瘤激酶(ALK)阳性的局部晚期和转移的非小细胞肺癌(NSCLC)。克唑替尼是酪氨酸激酶受体包括ALK、肝细胞生长因子受体(HGFR、c-Met)、ROS1和酪氨酸激酶(RON)的一种抑制剂。易位可影响ALK基因导致致癌融合蛋白的表达。ALK融合蛋白的形成导致激活和基因表达和增加细胞增殖有贡献信号的调节异常而生存肿瘤表达这些蛋

Brigatinib versus Crizotinib in ALK-Positive Non–Small-Cell Lung Cancer复制标题

吉美替尼与克唑替尼治疗ALK阳性非小细胞肺癌的比较

发表时间:2018-11-22

影响因子:70.7

作者: D.R. Camidge

期刊:N. Engl. J. Med.

A total of 275 patients underwent randomization; 137 were assigned to brigatinib and 138 to crizotinib. At the first interim analysis (99 events), the median follow-up was 11.0 months in the brigatinib group and 9.3 months in the crizotinib group. The rate of progression-free survival was higher with brigatinib than with crizotinib (estimated 12-month progression-free survival, 67% [95% confidence interval {CI}, 56 to 75] vs. 43% [95% CI, 32 to 53]; hazard ratio for disease progression or death, 0.49 [95% CI, 0.33 to 0.74]; P<0.001 by the log-rank test). The confirmed objective response rate was 71% (95% CI, 62 to 78) with brigatinib and 60% (95% CI, 51 to 68) with crizotinib; the confirmed rate of intracranial response among patients with measurable lesions was 78% (95% CI, 52 to 94) and 29% (95% CI, 11 to 52), respectively. No new safety concerns were noted. Among patients with ALK-positive NSCLC who had not previously received an ALK inhibitor, progression-free survival was significantly longer among patients who received brigatinib than among those who received crizotinib. (Funded by Ariad Pharmaceuticals; ALTA-1L ClinicalTrials.gov number, NCT02737501.).

译文

共有275名患者接受了随机化治疗;137名患者被分配到布里加汀组,138名患者被分配到克里佐替尼组。在第一次中期分析(99个事件)中,Brigatinib组的中位随访时间为11.0个月,Crizotinib组为9.3个月。Brigatinib组无进展生存率高于Crizotinib组(估计12个月无进展生存率,67%[95%可信区间{Ci},56-75]vs.43%[95%可信区间,32-53];疾病进展或死亡的危险比,0.49[95%可信区间,0.33-0.74];对数秩检验p<0.001)。brigatinib和crizotinib的客观确诊率分别为71%(95%ci,62~78)和60%(95%ci,51~68);可测量病变患者的颅内确诊率分别为78%(95%ci,52~94)和29%(95%ci,11~52)。没有发现新的安全问题。在以前没有接受alk抑制剂的alk阳性nsclc患者中,接受brigatinib的患者的无进展生存期明显长于接受crizotinib的患者。(由Ariad Pharmaceuticals资助;alta-1l clinicaltrials.gov编号,NCT 0273750)。