英文药名：Alectinib(Alectinib Hydrochloride Capsule) 中文药名：盐酸阿雷替尼胶囊 生产厂家：中外制药 アレセンサカプセル150mg 类别名称 抗肿瘤药/ALK注1）抑制剂 注1:ALK：间变性淋巴瘤激酶 盐酸阿雷替尼胶囊Alectinib(Alectinib Hydrochloride/AP26113)为新一代抗癌新药，在日本批准上市。突破性肺癌治疗药物 商標名 ALECENSA 一般名 アレクチニブ塩酸塩 (Alectinib Hydrochloride)(JAN) 化学名 9-Ethyl-6,6-dimethyl-8-［4-(morpholin-4-yl)piperidin-1-yl］-11-oxo-6,11-dihydro-5H-benzo［b］carbazole-3-carbonitrile monohydrochloride 構造式 分子式 C30H34N4O2・HCl 分子量 519.08 性　状 它是一种白色粉末与白色粉末黄色发红或质量。它是易溶略微2,2,2-三氟乙醇，乙醇（99.5），以溶解，不溶于水的小乙腈和丙酮非常轻微。 熔点 约302℃（分解） 审批条件 1.由于临床试验的情况下在日本是非常有限的，上市后，直到一定数量案件的数据被集成，通过实施的所有情况下，使用效果的调查，该药物以及了解病人使用的背景资料，搜集有关这种药物的安全性和有效性的数据在年初，采取必要措施，正确使用此药。 2.本剤药物，诊断肺癌，施用是熟悉的化疗，以便它药店下进行只存在一个医生，医疗机构和管理药剂师可完全管理也这种药物的风险。 药效药理 在ALK融合基因阳性的非小细胞肺癌，ALK酪氨酸激酶活性异常上升，并参与恶性转化和肿瘤的生长。 1.抗肿瘤效果 Arekuchinibu和主要代谢物（M-4）抑制人的非小细胞肺癌的来自ALK融合基因阳性的NCI-H2228细胞系的细胞生长。此外，Arekuchinibu，在NCI-H2228细胞系皮下注入严重联合免疫缺陷的小鼠，表现出对肿瘤生长的抑制效果。 2.作用机序 Arekuchinibu是通过抑制ALK酪氨酸激酶活性，抑制ALK融合基因阳性的肿瘤细胞的生长。 适应病症 〇对不能手术切除的晚期或ALK融合复发基因阳性非小细胞肺癌 用法用量 成人每日口服给药两次，每次一次150毫克 包装规格 胶囊： 150毫克*28粒（PTP 14粒×2） 150毫克*14粒/瓶 150毫克*98粒/瓶 生产厂商 中外制药有限公司 注：以上中文资料仅供参考，使用以原处方为准：http://www.info.pmda.go.jp/go/pack/4291032M3021_1_02/ 新型抗肿瘤靶向新药alectinib获日本批准 针对间变性淋巴瘤激酶 (ALK)阳性的非小细胞肺癌的最新靶向治疗药物 alectinib 首次获日本批准。该抗肿瘤药将由罗氏制药的分公司 Chugai推向日本市场，并于今年晚些时候正式面市。 在美国，FDA已批准抗肿瘤药alectinib用于克唑蒂尼治疗后发生进展的 ALK 阳性非小细胞肺癌患者的治疗，并授予该药突破性疗法称号。克唑蒂尼是首个ALK阳性非小细胞肺癌的靶向治疗药物，2011年8月在美国获批。 从那以后，在美国又有另一种特异性靶向抗肿瘤药被批准用于这类患者的治疗。4月，FDA提前批准ceritinib用于以前应用克里唑蒂尼治疗过的、ALK 阳性非小细胞肺癌患者的治疗。 日本卫生部、劳动和福利局批准该抗肿瘤药是基于在日本进行的I期和II期 AF-001JP临床试验的积极结果，该研究达到了缓解率大于90%的主要终点。罗氏公司指出，正在进行中的临床试验结果将用于世界其他地区的申请。Chugai还将与罗氏另一个分公司Ventana医疗合作进行Alectinib的全球性III期试验。 上述在日本的试验涉及晚期、复发或不能切除的、已经应用过至少一种化疗方案的、ALK阳性非小细胞肺癌患者。该试验分为两个部分。I期试验包括 24位患者，评估了上述抗肿瘤药的安全性、耐受性和药动学参数，确定了推荐剂量（300mg 口服，一天2次）。 II期试验包括46位患者，评估了推荐剂量的疗效和安全性。在该研究中，alectinib 组患者的缓解率为93.5%。此外，12个月时患者的无进展生存率为83%。 参与试验的70位患者中，14位有脑转移，其中9位患者12个月内没有中枢神经症状或系统进展。Roche指出，这些患者很难应用其他药物治疗，他们将继续研究这一问题。 Alectinib 的早期试验显示其对脑转移的治疗有效，表明该药能被大脑摄取。血脑屏障阻止分子影响大脑的其中一种方法是将其主动排出血脑屏障，这一过程叫做主动外排。该公司指出，主动外排系统不能识别alectinib，这意味着该抗肿瘤药可以进出脑组织。 ALECENSA Capsule（Alectinib hydrochloride） ALECENSA Capsule 150mg（アレセンサカプセル150mg）  Brand name : ALECENSA Capsule 150mg 　Active ingredient: Alectinib hydrochloride 　Dosage form: white to yellowish white, long diameter: approximately 19 mm 　Print on wrapping: アレセンサ150mg Effects of this medicine This medicine suppress cancer cell growth by selective inhibition of ALK fusion protein essential for cancer cell growth. It is usually used to treat ALK fusion gene-positive unresectable, recurrent or advanced non-small cell lung cancer. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines. If you have interstitial lung disease or have a history of it. If you have liver dysfunction. •If you are pregnant, possibly pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is <<to be written by a healthcare professional>> •In general, for adults, take 2 capsules (300 mg of Alectinib) twice a day. Strictly follow the instructions. •If you miss a dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time. •If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist. •Do not stop taking this medicine unless your doctor instructs you to do so. The disease may become worse by discontinuing the medicine, or adjusting the dose on your own judgment because you feel better. Precautions while taking this medicine •This medicine may cause serious adverse reactions. You should be informed of precautions, etc. until you fully understand them. •Since this medicine may cause interstitial lung disease, chest CT examination will be performed. Pulmonary function test may be performed, if needed. •Since this medicine may cause liver dysfunction or blood disorder (neutropenia, leukopenia, etc.), periodic blood test will be performed while taking this medicine. •Avoid pregnancy if you have possibility of it. Possible adverse reactions to this medicine The most commonly reported adverse reactions include taste disorder and rash. If any of these symptoms occur, consult with your doctor or pharmacist. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •shortness of breath, breathing difficulty, dry cough, fever [interstitial lung disease] •yellowing of the skin and the white of eyes, darkly-colored urine, nausea, vomiting, loss of appetite, general malaise, itch [liver dysfunction] •fever, sore throat [neutropenia, leukopenia] •severe stomachache, nausea, vomiting [perforation of the digestive tract] •chest pain, chest constriction, chest tightness, severe leg pain, abdominal bloating, severe stomachache, nausea, vomiting, vomiting of blood, bleeding, anesthesia [thromboembolism] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of the reach of children. Store at room temperature (1 to 30°C), away from direct sunlight and moisture. •Discard the remainder. Do not store them. Ask the pharmacist and the medical institution how to discard them. Chugai Pharmaceutical Co., Ltd.Internal Published: 11/2015 The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.