Adis, Level 1, 5 The Warehouse Way, Northcote, 0627, Auckland, New Zealand,
Drugs. 2014 Jul;74(11):1285-91. doi: 10.1007/s40265-014-0251-3.
Ceritinib is an oral anaplastic lymphoma kinase (ALK) inhibitor developed by Novartis for the treatment of tumours characterised by genetic abnormalities in ALK. ALK is a member of the insulin receptor family of tyrosine kinases that can become oncogenic when fused to other proteins. Ceritinib has been approved in the US under 'Breakthrough Therapy' designation for the second-line treatment of ALK-positive non-small cell lung cancer (NSCLC). Regulatory submissions have also been made in the EU and other countries. Phase III development is ongoing worldwide to evaluate ceritinib both as a first- and second-line therapy for ALK-positive NSCLC. This article summarizes the milestones in the development of ceritinib leading to this first approval for the treatment of patients with ALK-positive metastatic NSCLC who have progressed on or are intolerant to crizotinib.
塞瑞替尼是诺华公司开发的一种针对间变性淋巴瘤激酶（ALK）的口服抑制剂，用于治疗具有 ALK 基因异常的肿瘤。ALK 是胰岛素受体家族的一种酪氨酸激酶，当其与其他蛋白融合时可致癌。塞瑞替尼已被美国食品和药物管理局（FDA）授予“突破性疗法”认定，用于二线治疗 ALK 阳性非小细胞肺癌（NSCLC）。该药在欧盟和其他国家的监管申请也已提交。全球范围内正在进行 III 期临床试验，以评估塞瑞替尼作为一线和二线治疗 ALK 阳性 NSCLC 的疗效。本文总结了塞瑞替尼的开发历程中的重要里程碑，该药由此获得批准，用于治疗接受克唑替尼治疗后进展或不耐受克唑替尼的 ALK 阳性转移性 NSCLC 患者。
