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Review Article

恩曲替尼：一种新的选择性酪氨酸激酶抑制剂，批准用于治疗患有NTRK融合阳性，复发性或晚期实体瘤的儿科和成人患者

卷 29, 期 15, 2022

发表于: 01 April, 2022

页: [2602 - 2616] 页: 15

弟呕挨: 10.2174/0929867328666210914121324

价格: $65

摘要

背景：恩曲替尼是一种高效的ATP竞争性和选择性酪氨酸激酶抑制剂 - Trk ABC，ALK和ROS1。它由罗氏公司开发，并于2019年在日本首次获得批准，用于治疗NTRK融合阳性，复发性或晚期实体瘤的儿科和成人患者。2019年8月，恩曲替尼加速获得美国FDA对这一适应症的批准。它也是第一个FDA批准的药物，旨在同时针对NTRK和ROS1。 目的：总结近期新批准的选择性酪氨酸激酶抑制剂恩曲替尼的合成、作用机制及临床试验。 方法：对新型高效小分子恩曲替尼的研究进行文献综述。 结论：基于三项临床研究（ALKA，STARTRK-1和STARTRK-2）的Entrectinib耐受性良好, 全性可控。它在与 NTRK 融合阳性或 ROS1+ NSCLC 相关的复发性或晚期实体瘤中诱导了具有临床意义的反应。而且它对中枢神经系统转移患者显示出实质性的疗效。

关键词: 恩曲替尼，茚达唑苯甲酰胺，Trk ABC，ALK，ROS1抑制剂，NTRK融合阳性肿瘤。

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