...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Drugs of today: Medicamentos de actualidad >Osimertinib for the treatment of patients with EGFR mutation-positive non-small cell lung cancer
【24h】

Osimertinib for the treatment of patients with EGFR mutation-positive non-small cell lung cancer

机译：Osimertinib用于治疗EGFR突变阳性非小细胞肺癌的患者

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

Epidermal growth factor receptor (EGFR) mutations, mostly seen in exon 19 or exon 21, are present in roughly 50% of patients with advanced non-small cell lung cancer (NSCLC) of Asian ethnicity compared with 12% in Caucasians. EGFR-mu toted NSCLC patients have an increased sensitivity to EGFR tyrosine kinase inhibitors (TKIs), such as erlotinib, gefitinib or afatinib, showing superior response, progression-free survival and overall survival rates with EGFR-TKIs than with platinum doublet chemotherapy, which makes EGFR-TKIs the standard of care in this subgroup of NSCLC patients. This has been the most important step toward molecular-guided precision therapy for NSCLC. Despite the initial rapid and durable clinical responses, acquired resistance to EGFR-TKIs has been found to eventually develop in most cases, with disease progression observed mostly within 9-12 months after treatment. One of the most important mechanisms for resistance to EGFR-TKI therapy is the substitution of threonine to methionine (T790M) on exon 20 of the EGFR gene, which occurs in 49% to 60% of patients. Osimertinib mesylate (formerly AZO-9291) is a potent third-generation TKI which irreversibly inhibits mutated EGFR alleles, including T790M. This review summarizes osimertinib's pharmacology, pharmacokinetics, safety, side effects and clinical utility in the treatment of EGFR-mutated advanced NSCLC.
机译：表皮生长因子受体（EGFR）突变主要见于外显子19或外显子21，在亚裔晚期非小细胞肺癌（NSCLC）患者中约有50%存在这种突变，而在白种人中只有12%。EGFR-mu-toted NSCLC患者对EGFR酪氨酸激酶抑制剂（TKIs）的敏感性增加，如厄洛替尼、吉非替尼或阿法替尼，与铂双联化疗相比，EGFR-TKIs显示出更好的反应、无进展生存率和总生存率，这使得EGFR-TKIs成为该亚组NSCLC患者的标准治疗。这是NSCLC分子导向精确治疗最重要的一步。尽管最初的临床反应迅速而持久，但已发现大多数病例最终会产生对EGFR-TKIs的获得性耐药性，大多数患者在治疗后9-12个月内观察到疾病进展。对EGFR-TKI疗法产生耐药性的最重要机制之一是，EGFR基因外显子20上的苏氨酸替换为蛋氨酸（T790M），49%到60%的患者出现这种情况。甲磺酸欧西美替尼（以前称为AZO-9291）是一种有效的第三代TKI，可不可逆地抑制突变的EGFR等位基因，包括T790M。本文综述了奥西米替尼治疗EGFR突变晚期非小细胞肺癌的药理学、药代动力学、安全性、副作用和临床应用。

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