Novartis’ Ceritinib (Trade Name: Zykadia, previously known as LDK378, Chinese Name:色瑞替尼), an oral selective inhibitor of anaplastic lymphoma kinase (ALK),  was approved four months ahead of schedule on April 29, 2014 by the U.S. Food And Drug Administration (FDA) to treat patients with anaplastic lymphoma kinase-positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who were previously treated with Pfizer’s Xalkori (Crizotinib), the only other approved ALK tyrosine kinase inhibitor.

2014年4月29日，美国FDA批准Zykadia (色瑞替尼, ceritinib， LDK378)用于治疗晚期转移性非小细胞肺癌(NSCLC)。Zykadia是一种间变性淋巴瘤激酶(ALK)酪氨酸激酶抑制剂，它可以阻断促癌蛋白。这款药物适用于之前接受过克唑替尼（Crizotinib）治疗的转移性ALK阳性NSCLC患者，克唑替尼是仅有的另一款ALK酪氨酸激酶抑制剂.

Chemical Synthesis of Zykadia (Ceritinib, LDK378), Novartis’ ALK inhibitor for ALK+ Non-small Lung Cancer Treatment  诺华晚期非小细胞肺癌药物色瑞替尼(Zykadia)的化学合成

Trade Name：Zykadia
Generic Name：ceritinib
Synonym：LDK378
Chemical Name:5-Chloro-N2-[2-isopropoxy-5-methyl-4-(4-piperidinyl)phenyl]-N4-[2-(isopropylsulfonyl)phenyl]-2,4-pyrimidinediamine
CAS number：1032900-25-6
Mechanism of Action:Anaplastic lymphoma kinase inhibitor
Clinical Trail Data:among 163-treated patients, Zykadia achieved an overall response rate (ORR) of 54.6% and a median duration of response (DOR) of 7.4 months
Dosage and Administration:750 mg orally once daily
Date of Approval: April 29, 2014
Indication：ALK positive non-small cell lung cancer (ALK+ NSCLC)
Company:Novartis Pharmaceuticals Corporation

商品名：Zykadia
通用名：色瑞替尼 (ceritinib)
曾用名：LDK378
适应症：ALK阳性转移性非小细胞肺癌
剂型规格：本品为胶囊剂，推荐剂量为750mg/天
作用机理：ceritinib是ALK抑制剂，对表达EML4-ALK、NPM-ALK融合蛋白的细胞有抑制作用，能够克服crizotinib耐药性。
临床试验：一项开放标签试验入组了163例crizotinib耐药或不耐受的患者，总应答率为54.6%（完全应答1.2%+部分应答53.4%），持续应答时间为7.4个月
审批分类：突破性药物+优先审评+加速批准+孤儿药
批准日期：2014年4月29日
药企：诺华