英文药名：KADCYLA Powder for Infusion(ado-trastuzumab emtansine)   中文药名：曲妥珠单冻干粉注射剂 生产厂家：罗氏制药 药品介绍 2013年11月21日，罗氏（Roche）抗体偶联药物Kadcyla（trastuzumab emtansine，T-DM1）获欧盟委员会（EC）批准上市 注射用KADCYLA(ado-曲妥珠单抗emtansine)，为静脉使用 作用机制 Ado-曲妥珠单抗emtansine是一种靶向HER2抗体药物结合物。抗体是人源化抗-HER2 IgG1，曲妥珠单抗。小分子细胞毒素，DM1，是一种微管抑制剂。结合至HER2受体的亚结构区IV，ado-曲妥珠单抗emtansine  进行受体-介导内化和随后溶酶体降解，导致含DM1细胞毒降解产物的细胞内释放。DM1结合至微管蛋白破坏细胞内微管网络，导致阻止细胞周期和凋亡性细胞死亡。此外，体外研究已证明与曲妥珠单抗相似，ado-曲妥珠单抗emtansine抑制HER2受体信号，介导抗体-依赖细胞介导细胞毒性和抑制过表达HER2人乳癌细胞HER2细胞外结构区的脱落。 适应证和用途 KADCYLA是一种靶向HER2抗体和微管抑制剂结合物适用于，作为单药，为有HER2-阳性，转移乳癌，既往接受曲妥珠单抗和一种紫衫烷类，分开或联合应用患者的治疗。患者应有以下任一情况： （1）对转移疾病以前接受治疗，或 （2）完成辅助治疗期间或6个月内疾病复发。 剂量和给药方法 （1）只为静脉输注。不要静推注或丸注。不要使用葡萄糖(5%)溶液。 （2）KADCYLA的推荐剂量是3.6mg/kg每3周(21-天周期)静脉输注给药直至疾病进展或不能接受毒性。不要给予剂量大于3.6mg/kg的KADCYLA。不要替代KADCYLA或用曲妥珠单抗。 （3）不良事件的处理(输注相关反应，肝毒性，左心室功能障碍，血小板减少，肺毒性或周围神经病变)可能需要暂时中断，减低剂量，或终止KADCYLA治疗。 剂型和规格 在单次使用小瓶冻干粉含100mg每小瓶或160mg每小瓶. 禁忌证 无。 警告和注意事项 （1）肺毒性：在被诊断有间质性肺病或肺炎患者中永久终止KADCYLA。 （2）输注相关反应，超敏性反应：输注期间和后监视体征和症状。如发生重要输注相关反应或超敏性反应，减慢或中断输注和给予适当医学治疗。对危及生命输注相关反应永久终止KADCYLA。 （3）血小板减少：每次给予KADCYLA前监视血小板计数。适当时调整剂量。 （4）神经毒性：监视体征和症状。对经受3或4级周围神经病变患者暂时不用给药。 （5）HER2检验：由有测试能力的实验室用FDA-批准的检验进行检验。 不良反应 用KADCYLA (n=884被治疗患者)最常见不良反应(频数> 25%)是疲乏，恶心，肌肉骨骼痛，血小板减少，头痛，转氨酶增加，和便秘。 在特殊人群中使用 （1）哺乳母亲：终止哺乳或终止KADCYLA考虑到药物对母亲的重要性。 （2）生殖潜能妇女：忠告女性关于预防和计划妊娠。鼓励患者参加母亲妊娠注册通过联系1-800-690-6720)。 Roche breast cancer drug Kadcyla approved by the European Union On November 21, 2013, the Roche antibody-conjugated drug Kadcyla (trastuzumab emtansine, T-DM1) was approved by the European Commission (EC) for use in previously accepted Herceptin (trastuzumab, trastuzumab, trastuzumab, And a taxane-based treatment of locally advanced or metastatic HER2-positive breast cancer that can not be surgically resected. Kadcyla was approved on the basis of clinical data from the international phase III EMILIA trial, which had previously received Herceptin (trastuzumab, trastuzumab) and a taxane (Herceptin) Treatment of HER2-positive metastatic breast cancer in patients with Kadcyla were compared with standard therapy. The data showed that Kadcyla significantly improved overall survival (OS, 30.9 months vs 25.1 months) and progression-free survival (PFS, 9.6 months vs 6.4 months) compared with standard therapy, and fewer The patient experienced a serious adverse event. Previously, Kadcyla has been approved by the FDA and the Japanese Ministry of Labor and Welfare (MHLW) in February and September this year for the treatment of unresectable or recurrent HER2-positive breast cancer. Kadcyla is the first antibody-conjugated drug (ADC) approved for the treatment of HER2-positive metastatic breast cancer. Currently, metastatic breast cancer (mBC) has no curable drugs, so treatment is designed to help patients survive as long as possible. The treatment of HER2-positive mBR includes targeting drugs and chemotherapy regimens. Some of the side effects associated with standard chemotherapy significantly affect the quality of life of the patient, and sometimes even the need for dressing or withdrawal. About Kadcyla: Kadcyla is a HER2 targeted therapy, a drug that is conjugated to Roche's trastuzumab and ImmunoGen's DM1 cytotoxic agent and has two anti-cancer properties: HER2 inhibition of trastuzumab and DM1 Of cytotoxicity. Streptozotocin and DMl were conjugated with a stable linker to deliver DMl to HER2-positive breast cancer cells. Roche has Kadcyla's global development and commercialization rights. At present, Roche is conducting several studies evaluating the potential of Kadcyla for potential additional use, including first-line therapy for HER2-positive metastatic breast cancer, for the treatment of early HER2-positive breast cancer and advanced HER2-positive gastric cancer. This article Department of pharmacists/medical experts original translation finishing, welcome to reprint! At the same time the procurement of domestic scientific research institutions can contact us: 2363244352.3330889895  http://www.medicines.org.uk/emc/medicine/28568 ----------------------------------------------- 产地国家: 德国 原产地英文商品名: KADCYLA Powder for Infusion 100MG/vial 原产地英文药品名: ADO﹣TRASTUZUMAB EMTANSINE 中文参考商品译名: KADCYLA冻干粉注射剂 100毫克/支 中文参考药品译名: 曲妥珠单抗 生产厂家中文参考译名: 罗氏 生产厂家英文名: Roche ----------------------------------------------- 产地国家: 德国 原产地英文商品名: KADCYLA Powder for Infusion 160MG/vial 原产地英文药品名: ADO﹣TRASTUZUMAB EMTANSINE 中文参考商品译名: KADCYLA冻干粉注射剂 160毫克/支 中文参考药品译名: 曲妥珠单抗 生产厂家中文参考译名: 罗氏 生产厂家英文名: Roche