新一代抗癌新药盐酸阿雷替尼胶囊ALECENSA(Alectinib Hydrochloride/AP26113)在日本批准上市。为肺癌突破性治疗药物
ALECENSA®(alectinib)胶囊，为口服使用
初次批准：2015
作用机制
Alectinib是一种酪氨酸激酶抑制剂靶向ALK和RET。在非临床研究，alectinib抑制ALK 磷酸化和ALK-介导的下游信号蛋白STAT3和AKT的激活，和在窝藏ALK 融合，扩增，或激活突变多种细胞系减低肿瘤细胞活力。Alectinib的主要活性代谢物，M4，显示相似体外效力和活性。Alectinib和M4显示体外和体内对多种ALK 酶突变型，包括有些用克里唑蒂尼已进展患者NSCLC肿瘤内鉴定的突变体，在移植携带ALK融合肿瘤的小鼠模型中，给予alectinib 导致抗肿瘤活性和延长生命，包括颅内植入来自有ALK-肿瘤细胞系小鼠模型。
适应证和用途
ALECENSA是一个激酶抑制剂适用为的治疗有间变性淋巴瘤激酶(ALK)-阳性，转移非小细胞肺癌(NSCLC)进展对或是对克里唑蒂尼耐受的患者的治疗。这个适应证是在加快审批下被批准根据肿瘤反应率和反应时间。继续批准这个适应证可能取决于在验证性试验中临床获益的验证和描述。
剂量和给药方法
600 mg口服每天2次。与食物给予ALECENSA。
剂型和规格
胶囊：150mg
禁忌证
无。
警告和注意事项
⑴ 肝毒性：监视肝实验室测试每2周治疗的头2个月期间，和任何治疗期间定期。严重ALT，AST，或胆红素升高情况中，不给，然后减低剂量，或永久地终止ALECENSA。
⑵间质性肺病(ILD)/肺炎：0.4%患者发生。被诊断ILD/肺炎患者立即不给ALECENSA和如已确定没有ILD/肺炎的其他潜在原因永久地终止。
⑶心动过缓：常规地监视心率和血压。如症状性，不给ALECENSA然后减低剂量，或永久地终止。
⑷严重肌痛和肌酸磷酸激酶(CPK)升高：发生分别在1.2%和4.6%患者。治疗的头一个月期间每2周评估CPK和在患者报告不解释肌痛，触痛，或乏力。在严重CPK升高情况中，不给，然后恢复或减低剂量。
⑸胚胎胎儿毒性：ALECENSA可能致胎儿危害。忠告有生殖潜能女性对胎儿潜在风险和使用有效避孕。
不良反应
最常见不良反应(发生率≥20%)是疲乏，便秘，水肿和肌痛。
特殊人群中使用
哺乳：不要哺乳喂养。
完整资料附件：
http://www.info.pmda.go.jp/go/pack/4291032M3021_1_02/
ALECENSA Capsule 40mg（アレセンサカプセル40mg） 
Brand name : ALECENSA Capsule 40mg
　Active ingredient: Alectinib hydrochloride
　Dosage form: pale purplish red to dull purplish red, long diameter: approximately 18 mm
　Print on wrapping: 
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 unresectable progressive / recurrent non-small cell lung cancer positive for ALK infusion gene.
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 300 mg of Alectinib (7 capsules of ALECENSA Capsule 40mg and 1 capsule of ALECENSA Capsule 20mg) at a time, twice a day.
This preparation (ALECENSA Capsule 40mg) contains 40 mg of Alectinib per capsule.
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
Revised: 10/2015
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.    部份中文盐酸阿雷替尼处方资料（仅供参考）
商品名：ALECENSA
英文名：Alectinib Hydrochloride
中文名：盐酸阿雷替尼胶囊
生产商：中外制药
药品介绍
新一代抗癌新药盐酸阿雷替尼胶囊ALECENSA(Alectinib Hydrochloride，アレセンサカプセル20mg)在日本批准上市。为肺癌突破性治疗药物.
アレセンサカプセル20mg／アレセンサカプセル40mg
药用类别名称
抗恶性肿瘤药物/lk注 1) 抑制剂
注 1) ALK: 再生性淋巴瘤激酶 (未分化淋巴瘤激酶)
批准日期：2015年11月
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：
白色到黄色的红色是一种带有白色粉末或肿块的粉末。微溶于2, 2, 2-三氟乙醇, 很难溶于乙醇 (99.5), 水, 几乎不溶于乙腈和丙酮。
熔点
约 302°c (拆卸)
药用药理学
在ALK融合基因阳性的非小细胞肺癌中, ALK酪氨酸激酶活性异常增强, 并参与癌变和肿瘤增殖。
1. 抗肿瘤作用
Arechinibu和主要代谢物(M-4)抑制了人的非小细胞肺癌NCI-H2228细胞系的细胞增殖, 这些细胞系来源于ALK融合基因阳性。此外, Arechienibu, 在重症复杂型免疫缺陷小鼠皮下移植NCI-H2228细胞系显示肿瘤生长的抑制作用。
2. 作用机制
Altininib 通过抑制ALK酪氨酸激酶活性来抑制ALK融合基因阳性肿瘤细胞的增殖。
适应症
·ALK融合基因阳性的非小细胞肺癌无法切除的进展和复发
用法与用量
通常情况下, 成人每天口服两次300毫克一次。
包装
胶囊
150毫克:28 胶囊(PTP14胶囊x2)
制造和销售来源
中外制药
ALECENSA Capsule 40mg（アレセンサカプセル40mg）
Brand name : ALECENSA Capsule 40mg
　Active ingredient: Alectinib hydrochloride
　Dosage form: pale purplish red to dull purplish red, long diameter: approximately 18 mm
　Print on wrapping:
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 unresectable progressive / recurrent non-small cell lung cancer positive for ALK infusion gene.
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 300 mg of Alectinib (7 capsules of ALECENSA Capsule 40mg and 1 capsule of ALECENSA Capsule 20mg) at a time, twice a day.
This preparation (ALECENSA Capsule 40mg) contains 40 mg of Alectinib per capsule.
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
Revised: 10/2015
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.