摘要

BGJ398, a potent and selective pan-FGFR antagonist, was prospectively evaluated in patients with metastatic urothelial carcinoma bearing a diverse array of FGFR3 alterations. Patients (N = 67) who were unable to receive platinum chemotherapy were enrolled. The majority (70.1%) had received two or more prior antineoplastic therapies. BGJ398 was administered orally at 125 mg/day on a 3 weeks on, 1 week off schedule until unacceptable toxicity or progression. The primary endpoint was the response rate. Among 67 patients treated, an overall response rate of 25.4% was observed and an additional 38.8% of patients had disease stabilization, translating to a disease control rate of 64.2%. The most common treatment-emergent toxicities were hyperphosphatemia, elevated creatinine, fatigue, constipation, and decreased appetite. Further examination of BGJ398 in this disease setting is warranted.Significance: BJG398 is active in patients with alterations in FGFR3, resulting in both reductions in tumor volume and stabilization of disease. Our data highlight putative mechanisms of resistance to the agent, which may be useful in following disease status. Cancer Discov; 8(7); 812-21. ©2018 AACR.This article is highlighted in the In This Issue feature, p. 781.

译文

BGJ398 是一种有效且选择性的泛 FGFR 拮抗剂,在患有多种 FGFR3 改变的转移性尿路上皮癌患者中进行了前瞻性评估。纳入无法接受铂类化疗的患者 (N = 67)。大多数人 (70.1%) 之前接受过两种或两种以上的抗肿瘤治疗。BGJ398 以 125 毫克/天口服给药,为期 3 周,休假 1 周,直到不可接受的毒性或进展。主要终点是反应率。在 67 名接受治疗的患者中,观察到总体反应率为 25.4%,另外 38.8% 的患者病情稳定,疾病控制率为 64.2%。最常见的治疗副作用是高磷血症、肌酐升高、疲劳、便秘和食欲下降。在这种疾病环境下,BGJ398 的进一步检查是必要的。意义: BJG398 在 FGFR3 改变的患者中是活跃的,导致肿瘤体积减少和疾病稳定。我们的数据突出了对该药剂的抗性的假定机制,这可能在以下疾病状态中有用。癌症迪斯科; 8 (7); 812-21。©2018 AACR。这篇文章在本期专题中突出显示,781 页。

fibroblast growth factor receptor

肿瘤 FGFR 临床研究术语
概述  :  

成纤维细胞生长因子受体(FGFR)属于跨膜受体酪氨酸激酶(RTK)家族,是成纤维细胞生长因子(FGF)的高亲和力受体,介导成纤维细胞生长因子传递入细胞质中。目前已经确定了由4种独立基因编码的FGFRs,即FGFR1-4。这些FGFR与其结合的配体可以诱导FGFR二聚化,启动级联反应,介导一些重要的生理过程,如胚胎发生,组织修复,伤口愈合和血管生成。有证据表明,FGF / FGFR途径的异常信号传导有可能引发人类恶性肿瘤的发病,包括尿路上皮癌,乳腺癌,子宫内膜癌,鳞状肺癌,卵巢癌和胆管癌。因此

Fibroblast   英 /'faɪbrə(ʊ)blæst/   美 /'faɪbrəblæst/

释    义   n. [基医] 纤维原细胞;纤维组织母细胞

例    句   In the present, there are fat cell transplantation, fibroblast transplantation and cartilage cell transplantation in the plastic surgery field. 目前涉及整形外科领域的主要是脂肪细胞移植、成纤维细胞移植和软骨细胞移植。

 

Growth   英 /grəʊθ/   美 /ɡroθ/

释    义   n. 增长;发展;生长;种植;复数 growths

同根词   grown adj. 长大的;成年的;长满某物的

               growing adj. 发展的;成长的

               grower n. 栽培者;生长物

               grown n. 生长;变成;栽培(grow的过去分词)

例    句   Whether in life which angle, I all at growth. 不论在生活的哪个角度,我都在成长。

 

Factor   英 /'fæktə/   美 /'fæktɚ/

释    义   n. 因素;要素;[物] 因数;代理人;vi. 做代理商;vt. 把…作为因素计入;代理经营;把…分解成

同根词   factory n. 工厂;制造厂;代理店

               factoring n. [数] 因子分解,[数] 因式分解;保付代理

               factorization n. [数] 因子分解;[数] 因式分解

               factoring v. 把…因素包括进去(factor的ing形式);

例    句   But this cannot be the only factor. 但这不可能是唯一的因素。

 

Receptor   英 /rɪˈseptə(r)/   美 /rɪˈseptər/

释    义   n. [生化] 受体;接受器;感觉器官

同根词   receptive adj. 善于接受的;能容纳的

               receptivity n. 接受能力;[生理] 感受性

               receptiveness n. 感受性;接受能力

例    句   Human tumor cells expressed high levels of growth factor and its receptor . 人类肿瘤细胞表达高水平的生长因子及其受体。

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