XALKORI Capsules(クリゾチニブ（Crizotinib）)

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XALKORI® (crizotinib)胶囊，口服

美国初始批准： 2011

适应证和用途
XALKORI是一种激酶抑制剂适用于有局部晚期或转移非小细胞肺癌(NSCLC)患者的治疗是当用一种FDA批准的检验变性淋巴瘤激酶(ALK)-阳性。(1) 这个适应症是基于反应率。没有可以得到的资料显示用XALKORI报道患者的结局或生存改善。

剂量和给药方法
（1）250 mg口服每天2次有或无食物。
（2）根据个体安全性和耐受性可能需要给药中断和/或剂量减低至200 mg口服每天2次，然后如需要进一步减低至250 mg口服每天1次。

剂型和规格
（1）XALKORI胶囊: 250 mg和200 mg.

禁忌证
无

警告和注意事项
（1）肺炎：严重，包括致命性，治疗-相关肺炎曾观察到。为指示性肺炎肺部症状监视患者。有治疗-相关肺炎诊断患者中永远终止。
（2）肝实验室异常：曾发生ALT和总胆红素同时升高。每月监视和当临床指示有2-4级升高患者用更频繁检验。当指示，暂时停止，减低剂量，或永远终止XALKORI。
（3）QT间隔延长：有病史或QTc延长倾向患者，或服用已知延长QT间隔药物, 应考虑监视心电图定期和电解质。
（4）ALK检验：为选择用ALKORI治疗患者需要用一种FDA批准的检验检测ALK-阳性NSCLC，适用于这个用途。
（5） 妊娠：当给予妊娠妇女时XALKOR可能致胎儿危害。

不良反应
最常见不良反应(≥25%)是视力障碍，恶心，腹泻，呕吐，水肿，和便秘。

为报告怀疑不良反应联系Pfizer Inc.电话1-800-438-1985或FDA电话1-800-FDA-1088或www.fda.gov/medwatch.

药物相互作用
（1）CYP3A抑制剂：避免XALKORI与强CYP3A抑制剂同时使用。
（2）CYP3A诱导剂：避免XALKORI与强CYP3A诱导剂同时使用。
（3）CYP3A底物：对共同给药药物主要被CYP3A代谢可能需要减低剂量。避免XALKORI与有狭窄治疗指数CYP3A底物同时使用。

如何供应/贮存和处置
250 mg胶囊
硬明胶胶囊有粉色不透明帽和体，帽上用黑墨汁印有“Pfizer”，体上“CRZ 250”；可得到：
60粒胶囊瓶： NDC 0069-8140-20
200 mg胶囊
硬明胶胶囊有粉色不透明帽和白色不透明体，帽上用黑墨汁印有“Pfizer”，体上“CRZ 200“可得到：
60粒胶囊瓶：NDC 0069-8141-20
贮存在室温20至25°C (68至77°F)；外出允许15°至30°C (59°至86°F)[见USP控制室温]。

FDA NEWS RELEASE
For Immediate Release: Aug. 26, 2011
Media Inquiries: Erica Jefferson, 301-796-4988
Consumer Inquiries: 888-INFO-FDA
FDA approves Xalkori with companion diagnostic for a type of late-stage lung cancer
Second targeted therapy approved with a test this year
The U.S. Food and Drug Administration today approved Xalkori (crizotinib) to treat certain patients with late-stage (locally advanced or metastatic), non-small cell lung cancers (NSCLC) who express the abnormal anaplastic lymphoma kinase (ALK) gene.
Xalkori is being approved with a companion diagnostic test that will help determine if a patient has the abnormal ALK gene, a first-of-a-kind genetic test called the Vysis ALK Break Apart FISH Probe Kit. It is the second such targeted therapy approved by the FDA this year.
This ALK gene abnormality causes cancer development and growth. About 1 percent to 7 percent of those with NSCLC have the ALK gene abnormality. Patients with this form of lung cancer are typically non-smokers. Xalkori works by blocking certain proteins called kinases, including the protein produced by the abnormal ALK gene. Xalkori is a pill taken twice a day as a single-agent treatment.
“The approval of Xalkori with a specific test allows the selection of patients who are more likely to respond to the drug” said Richard Pazdur, M.D., director of the Office of Oncology Drug Products in the FDA’s Center for Drug Evaluation and Research. “Targeted therapies such as Xalkori are important options for treating patients with this disease and may ultimately result in fewer side effects.”
Xalkori’s safety and effectiveness were established in two multi-center, single-arm studies enrolling a total of 255 patients with late-stage ALK-positive NSCLC. A sample of a patient’s lung cancer tissue was collected and tested for the ALK gene abnormality prior to study enrollment. The studies were designed to measure objective response rate, the percentage of patients who experienced complete or partial cancer shrinkage. Most patients in the studies had received prior chemotherapy.
In one study, the objective response rate was 50 percent with a median response duration of 42 weeks. In another, the objective response rate was 61 percent with a median response duration of 48 weeks.
The FDA based its approval of the Vysis ALK Break Apart FISH Probe Kit on data from one of the studies.
Xalkori was reviewed under the FDA’s priority review program, which provides for an expedited six-month review of drugs that may offer major advances in treatment or that provide a treatment when no adequate therapy exists.
Xalkori is being approved under the FDA’s accelerated approval program, which allows the agency to approve a drug to treat a serious disease based on clinical data showing that the drug has an effect on an endpoint that is reasonably likely to predict a clinical benefit to patients. The program is designed to provide patients with earlier access to promising new drugs, followed by further studies to confirm the drug’s clinical benefit.
Xalkori and the companion Vysis ALK Break Apart FISH Probe Kit were approved ahead of the drug’s Sept. 30, 2011, FDA review goal date and the companion diagnostics’ Sept. 28, 2011, review goal date.
“The trend in oncology research continues towards targeted therapies,” said Alberto Gutierrez, Ph.D., director of the Office of In Vitro Diagnostic Device Evaluation and Safety in the FDA’s Center for Devices and Radiological Health. “This test is an example of the important role companion diagnostics play in determining that the safest and most effective treatments are promptly delivered to patients living with serious and life-threatening diseases.”
The most common side effects reported in patients receiving Xalkori included vision disorders, nausea, diarrhea, vomiting, swelling (edema), and constipation. Vision disorders included visual impairment, flashes of light, blurred vision, floaters, double vision, sensitivity to light, and visual field defects. Xalkori use has also been associated with inflammation of the lung tissue (pneumonitis), which can be life-threatening. Patients with treatment-related pneumonitis should permanently stop treatment with Xalkori. The drug should not be used in pregnant women.
In July 2011, FDA issued a draft guidance industry on the agency’s policy for reviewing a companion diagnostic and the corresponding drug therapy. The guidance is currently available for public comment.
Xalkori is marketed by New York City-based Pfizer. The Vysis

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产地国家：美国
所属类别：抗癌药物 ->治疗肺癌药物
原产地英文药品名：
CRIZOTINIB
中文参考药品译名：
克卓替尼
原产地英文商品名：
XALKORI 200MG/CAP 60CAPS/BOTTLE
中文参考商品译名：
XALKORI 200毫克/胶囊 60胶囊/瓶
生产厂家英文名：
PFIZER
生产厂家中文参考译名：
辉瑞
该药品相关信息网址1：
http://www.xalkori.com/
曾用名：
未知
---------------------------------------------------------------
原产地英文药品名：
CRIZOTINIB
中文参考药品译名：
克卓替尼
原产地英文商品名：
XALKORI 250MG/CAP 60CAPS/BOTTLE
中文参考商品译名：
XALKORI 250毫克/胶囊 60胶囊/瓶
生产厂家英文名：
PFIZER
生产厂家中文参考译名：
辉瑞
该药品相关信息网址1：
http://www.xalkori.com/
曾用名：
未知

韩国上市的克卓替尼
항암제
잴코리TM캡슐 Xalkori TM capsules 200 mg, 250 mg

성분/함량
1캡슐당 크리조티닙 (별규) 200 mg,  250 mg

효능/효과
● 역형성 림프종 인산화효소 (ALK) 양성 국소 진행성 또는 전이성 비소세포폐암의 치료
● 이 약의 유효성은 반응률에 근거하였으며, 환자보고 결과 또는 생존기간의 개선을 입증한 자료는 없습니다.

용법/용량
● 이 약은 성인에게 250 mg 을 1일 2회 경구투여합니다.
● 이 약은 음식물과 관계없이 투여할 수 있으며, 캡슐제를 그대로 삼켜 복용하여야 합니다.
● 치료로 인한 임상적 이익이 지속되는 한 투여를 계속합니다.
● 복용을 잊은 경우, 다음 복용까지 남은 시간이 6시간 이상이면 환자가 기억한 즉시 복용해야 하며, 6시간 미만이면 복용하지 않습니다.
● 잊은 투여량을 보충하기 위해 2회 용량을 한꺼번에 복용해서는 안됩니다.

포장
200 mg: 60캡슐/블리스터
250 mg: 60캡슐/블리스터

日本上市的克卓替尼

ザーコリカプセル200mg／ザーコリカプセル250mg

有効成分に関する理化学的知見

一般名
クリゾチニブ（Crizotinib）

化学名
3-［（1R）-1-（2,6-Dichloro-3-fluorophenyl）ethoxy］-5-［1-（piperidin-4-yl）-1H-pyrazol-4-yl］pyridin-2-amine

分子式
C21H22Cl2FN5O

分子量
450.34

構造式
 

性状
本品は白色～微黄色の粉末である。N,N-ジメチルアセトアミドにやや溶けやすく、メタノール及びエタノール（95）にやや溶けにくく、アセトニトリルに溶けにくく、水にほとんど溶けない。本品は0.1mol/L塩酸試液に溶ける。

分配係数（log D）
1.65（pH7.4、1-オクタノール/水）

承認条件

1.
国内での治験症例が極めて限られていることから、製造販売後、一定数の症例に係るデータが集積されるまでの間は、全症例を対象に使用成績調査を実施することにより、本剤使用患者の背景情報を把握するとともに、本剤の安全性及び有効性に関するデータを早期に収集し、本剤の適正使用に必要な措置を講じること。

2.
本剤の投与が、肺癌の診断、化学療法に精通し、本剤のリスク等についても十分に管理できる医師・医療機関・管理薬剤師のいる薬局のもとでのみ行われるよう、製造販売にあたって必要な措置を講じること。

製造販売（輸入）
ファイザー株式会社

包装

ザーコリカプセル200mg：10カプセル（PTP）

ザーコリカプセル250mg：10カプセル（PTP）

原件处方附件：http://www.info.pmda.go.jp/go/pack/4291026M1023_1_01/