t). Avoid concomitant CYP3A substrates (eg, alfentanil, cyclosporine, ergots, fentanyl, pimozide, quinidine, sirolimus, tacrolimus) or CYP2C9 substrates (eg, phenytoin, warfarin) with narrow therapeutic indices; if unavoidable, reduce doses of these drugs. Avoid concomitant agents known to cause bradycardia (eg, beta-blockers, non-dihydropyridine CCBs, clonidine, digoxin).
Adverse Reaction(s)
Diarrhea, nausea, vomiting, abdominal pain, constipation, elevated transaminases, fatigue, decreased appetite; bradycardia, hepatotoxicity, ILD/pneumonitis, QTc prolongation, hyperglycemia.
How Supplied:
Caps—70
LAST UPDATED:
7/7/2014
晚期肺癌治疗药物Zykadia(Ceritinib, LDK378)获FDA批准
2014年4月29日，美国FDA批准Zykadia (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。
肺癌是因癌死亡的主要因素。根据美国国家癌症研究所提供的信息，今年美国预计有22.421万人将被确诊为肺癌，有15.92万人将死于这种疾病。大约85%的肺癌是NSCLC，这使其成为最常见的肺癌类型。然而，只有2-7%的NSCLC患者其ALK呈阳性。
Zykadia是第四款以突破性治疗药物资格获得FDA批准的药物。它比这款药物的处方药用户付费目标日期2014年8月24日相比，提前4个月获得批准，后者是FDA计划完成药物申请审评的预期日期。
FDA 授予Zykadia突破性治疗药物资格，优先审评及孤儿药资格，因为这款药物的申请者通过初步临床试验证据证明这款药物可能会提供一种相对现有治疗药物的实质性改善；这款药物在其申请提交时，在一种严重疾病治疗的安全性或有效性方面可能有显著改善，并且这款药物旨在治疗一种罕见疾病。
Zykadia的安全性及有效性基于一项由163名转移性ALK阳性NSCLC受试者参与的临床试验。所有受试者均以Zykadia治疗。结果显示，大约50%的受试者其肿瘤缩小，这种效果平均持续了大约7个月。
Zykadia的常见副作用包括消化道症状，如腹泻、恶心、呕吐和腹痛。肝酶增加、胰酶及葡萄糖水平增加等实验室异常也有被观察到。Zykadia由诺华上市销售。
商品名：Zykadia
通用名：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
药企：诺华
Zykadia™
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Generic name: Ceritinib
Chemocare.com uses trade names in all descriptions of drugs. Zykadia™ is the trade name for the generic chemotherapy drug ceritinib. In some cases, health care professionals may use the generic name ceritinib when referring to the trade drug Zykadia™.
Drug type: Zykadia™ is a targeted therapy. It is an oral tyrosine kinase inhibitor - (For more detail, see "How this drug works," below.)
What this drug is used for:
For the treatment of non-small cell lung cancer that is caused by a defect in a gene called ALK (anaplastic lymphoma kinase). The cancer must be (ALK)-positive as indicated by an FDA-approved test.
Note: If a drug has been approved for one use, physicians may elect to use this same drug for other problems if they believe it may be helpful.
How this drug is given:
•Zykadia™ is a capsule, taken by mouth: the standard starting dose is 5 capsules, once daily. It should be taken on an empty stomach (do not eat for 2 hours before and 2 hours after your dose).
•Take Zykadia™ exactly as prescribed.
•Swallow Zykadia™ capsules whole. Do not crush, dissolve or open capsules.
•Do not change your dose or stop Zykadia™ unless your health care provider tells you to.
•If you miss a dose, take it as soon as you remember. If your next dose is due within 12 hours, then skip the missed dose. Take the next
