Role of osimertinib in the treatment of EGFR-mutation positive non-small-cell lung cancer
Role of osimertinib in the treatment of EGFR-mutation positive non-small-cell lung cancer
复制标题
DOI：
10.2217/fon-2018-0626
复制
发表时间：
2019-03-01
期刊：
影响因子：
3.3
通讯作者：
Ramalingam, Suresh S.
中科院分区：
文献类型：
--
作者：
Carlisle, Jennifer W.;Ramalingam, Suresh S.
EGFR突变发生在约10-35%的非小细胞肺癌（NSCLC）患者中。奥希替尼是第三代口服EGFR小分子抑制剂，对L 858 R和外显子19缺失中常见的靶向激活EGFR突变具有活性;它还抑制T790 M突变。最初开发并批准用于治疗对T790 M通路激活介导的EGFR抑制的获得性耐药。最近，FLAURA试验显示，与第一代EGFR酪氨酸激酶抑制剂吉非替尼或厄洛替尼相比，奥希替尼可显著改善无进展生存期;这导致其被美国FDA和欧洲药品管理局（EMA）批准为一线治疗。正在进行的研究将确定奥希替尼的耐药机制、新型联合治疗方法和在早期NSCLC中的作用。
Mutations in the EGFR occur in approximately 10-35% of non-small-cell lung cancer (NSCLC) patients. Osimertinib is a third-generation oral small molecule inhibitor of EGFR, active against the common targetable activating EGFR mutations in L858R and exon 19 deletion; it also inhibits the T790M mutation. It was initially developed and approved for the treatment of acquired resistance to EGFR inhibition mediated by the T790M pathway activation. Recently, the FLAURA trial showed significantly improved progression-free survival with osimertinib compared with the first generation EGFR tyrosine kinase inhibitors gefitinib or erlotinib; this has led to its approval by US FDA and European Medicines Agency (EMA) as frontline therapy. Ongoing studies will define the resistance mechanisms to osimertinib, novel combination approaches and role in earlier stages of NSCLC.