英文药名：XALKORI Capsules（Crizotinib）   中文药名：克里唑蒂尼胶囊 生产厂家：辉瑞日本公司 ザーコリカプセル200mg／ザーコリカプセル250mg 药用类别名称 抗肿瘤药物/酪氨酸激酶抑制剂 批准日期：2012年5月 商標名 XALKORI Capsules 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 本品为白色至细黄色粉末。 n, 微溶于 n-dimethylacetamide, 它几乎不溶于甲醇和乙醇 (95), 几乎不溶于乙腈, 几乎没有融化成水。 本产品融为0.1 摩尔/升盐酸试验溶液。 分配系数 (日志 D) 1.65 (ph7.4, 1-辛醇/水) 审批标准 *制定药物风险管理计划并适当实施。 *表达融合基因阳性非小细胞肺癌 1. 由于日本的临床试验病例极为有限, 在生产和销售之后, 积累了一定数量的病例数据, 并通过对所有病例进行使用结果调查, 掌握了使用该制剂的患者的背景资料。 在早期收集有关该制剂的安全性和有效性的数据, 并采取必要措施适当使用该制剂。 2. 本药物的管理采取必要的生产和销售措施, 只有在对肺癌、化疗和这种药物的风险进行适当管理的药房下进行, 如医生、医疗机构和管理药剂师。 *ROS1 融合基因阳性非小细胞肺癌 这种药物的管理是采取必要的措施, 生产和销售, 因此, 它只是在药房的诊断肺癌是熟悉的化疗, 并有可能管理的风险等, 这药足够的, 只有在药店的医生, 医疗机构。 药用药理学 1. 抗肿瘤作用 Crizotinib, 通过易位/反演的人非小细胞肺癌衍生nci-h3122和nci-h2228细胞株表达的言下融合蛋白, 以及ros1基因的易位, 抑制了 ROS1融合蛋白表达的人非小细胞肺癌衍生 hcc78 细胞株的增殖。 此外, 在免疫缺陷小鼠移植nci-h3122细胞株, 以抑制肿瘤的生长。 2. 作用机制 Crizotinib是一种酪氨酸激酶抑制剂, 可用于HGFR, 肝细胞生长因子受体(C-满足/), ROS1和 Recepteur d ' 起源泰斯 (RON)。 Crizotinib被认为抑制肿瘤的生长, 抑制了 ROS1 融合蛋白的酪氨酸激酶活性, 是 ROS1 的致癌突变体。 适应症 非小细胞肺癌的吻合融合基因阳性切除与复发 ROS1 融合基因阳性切除与复发的非小细胞肺癌 用法和用量 成年；每天一次，每次250mg。此外, 适当减少的情况下, 病人。 包装 胶囊剂 200mg:10粒(PTP) 250mg:10粒(PTP) 制造和销售 (进口) 辉瑞公司 注：以上中文资料不够完整，使用者以原资料为准。 完整说明书附件：http://www.info.pmda.go.jp/go/pack/4291026M1023_1_12/ XALKORI（crizotinib capsule，中文药名 克里唑蒂尼胶囊）是一种口服酪氨酸激酶受体抑制剂，为6年来第一个治疗肺癌的新药 New release of anti-malignant oncology Agent "Zakori ® Capsule 200mg/250mg" -ALK fusion gene-positive adapted to non-small cell lung cancer May 29, 2012 (Tue), undifferentiated lymphoma kinase (ALK), the efficacy of the non-malignant cell lung cancer (NSCLC: Non-small cell Lung Cancer), in effect, anti-malignancy/ tyrosine kinase inhibitor "Zacolicapsel 200mg/250mg" (General Name: Crizotinib, hereinafter, "Zakori") has been released. In just five years from the publication of the ALK Fusion gene discovery, being able to deliver this medicine to patients with limited treatment options was a great pleasure for us as a company, and I would like to thank all the people who have helped us to achieve that. Zakori Overview Product Name Zakori®Capsule 200mg/250mg (Xalkori ® Capsules) General name Crizotinib (crizotinib) Classified anti-malignant tumor agent/tyrosine kinase inhibitor Non-small cell lung cancer with ALK and recurrence of a positive and effective fusion gene Usage/dosage Usually, the adult is administered once 250mg twice a day as a crizotinib. In addition, I will be appropriately reduced by the condition of the patient. Manufacturing and Sales Pfizer Corporation Drug Zacolicapsel 200mg (200mg1 capsule) Zacolicapsel 250mg (250mg1 capsule) Production and sales approval date March 30, 2012 Drug price Listing date May 29, 2012 Promotion of proper use Pfizer considers the accumulation of more clinical data to be more secure and effective for use by Zakori, and, in accordance with the approval conditions of this agent, through the survey of specific use results after manufacturing and sales (all cases survey) We collect safety and efficacy data at an early stage and take the necessary measures for proper use of this agent. In the case of all cases, we will confirm the facility and physician requirements, provide proper use information by Mr before the delivery of this medicine, and require regular information collection visits after delivery. For medical professionals, the appropriate use guide will be prepared for patients, and the Doctor who is prescribed this medicine can explain the safety measures to patients and their families. In addition, the side effects information that is collected after the sale will be published in the site "Pfizer for PROFESSIONALS" for our medical personnel (updated once a week).