...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Clinical cancer research: an official journal of the American Association for Cancer Research >Idelalisib: First-in-Class PI3K Delta Inhibitor for the Treatment of Chronic Lymphocytic Leukemia, Small Lymphocytic Leukemia, and Follicular Lymphoma
【24h】

Idelalisib: First-in-Class PI3K Delta Inhibitor for the Treatment of Chronic Lymphocytic Leukemia, Small Lymphocytic Leukemia, and Follicular Lymphoma

机译：Idelalisib：一流的PI3K Delta抑制剂，用于治疗慢性淋巴细胞性白血病，小淋巴细胞性白血病和滤泡性淋巴瘤

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Idelalisib [Zydelig (Gilead Sciences, Inc.), also known as CAL-101 and GS-1101] was approved in 2014 in the United States and European Union for the treatment of three indolent B-cell neoplasms: relapsed/refractory chronic lymphocytic leukemia (CLL, in combination with rituximab), relapsed follicular lymphoma, and relapsed small lymphocytic lymphoma (as monotherapy). Furthermore, it was approved in the European Union as first-line therapy for poor-prognosis CLL with 17p deletions or TP53 mutations and in patients unsuitable for chemoimmunotherapy. Idelalisib is an orally bioavailable ATP-competitive kinase inhibitor that targets the PI3K p110 isoform delta (PI3K delta) with high potency and selectivity. PI3K delta is hyper-activated in B-cell malignancies and plays a pivotal role in the B-cell receptor pathway, a key oncogenic driver in B-cell malignancies. The near exclusive expression of the PI3K delta isoform in hematopoietic cells and the selectivity of idelalisib for the PI3K delta isoform are essential for its efficacy and tolerability, even in elderly patients unfit for chemotherapy. Idelalisib is the first PI3K inhibitor approved by the regulatory agencies; this approval will change the treatment landscape of indolent B-cell malignancies. (C) 2015 AACR.
机译：Idelalisib [Zydelig（Gilead Sciences，Inc.），也称为CAL-101和GS-1101]于2014年在美国和欧盟获得批准，用于治疗三种惰性B细胞肿瘤：复发/难治性慢性淋巴细胞性白血病（CLL，合并利妥昔单抗），复发性滤泡性淋巴瘤和复发性小淋巴细胞性淋巴瘤（作为单一疗法）。此外，它已被欧盟批准为预后不良的伴有17p缺失或TP53突变的CLL以及不适合化学免疫治疗的患者的一线治疗。 Idelalisib是一种口服生物可利用的ATP竞争性激酶抑制剂，可高效靶向PI3K p110亚型delta（PI3K delta）。 PI3Kδ在B细胞恶性肿瘤中高度活化，并在B细胞受体途径中发挥关键作用，而B细胞受体途径是B细胞恶性肿瘤的关键致癌驱动因素。即使在不适合化疗的老年患者中，PI3Kδ亚型在造血细胞中的近乎排他性表达以及艾达利西布对PI3Kδ亚型的选择性对于其疗效和耐受性也至关重要。艾达拉西布是首个被监管机构批准的PI3K抑制剂。该批准将改变惰性B细胞恶性肿瘤的治疗方式。 （C）2015 AACR。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号