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Alectinib是一种口服间变性淋巴瘤激酶(anaplastic lymphoma kinase,ALK)抑制剂,能选择性抑制ALK和转染重排(rearranged during transfection,RET)激酶。2015年12月由美国FDA加速批准上市,用于治疗ALK阳性、转移性非小细胞肺癌(NSCLC)进展或不能耐受克唑替尼(crizotinib)治疗的患者。临床试验表明其疗效较好,主要不良反应为乏力、便秘、水肿、肌肉疼痛和咳嗽等。现对其作用机制、药动学、临床研究及不良反应等做一综述。
Alectinib is an oral anaplastic lymphoma kinase (ALK) inhibitor that selectively inhibits ALK and rearranged during transfection (RET) kinases. December 2015 Approved by the U.S. FDA to speed up the market for the treatment of patients with ALK-positive, metastatic non-small cell lung cancer (NSCLC) progression or who can not tolerate crizotinib. Clinical trials show that its efficacy is better, the main adverse reactions were fatigue, constipation, edema, muscle pain and cough. Now its mechanism of action, pharmacokinetics, clinical studies and adverse reactions to do a review.