部份中文曲妥珠单抗处方资料（仅供参考）
通用名：曲妥珠单抗注射剂
英文名：KADCYLA（ado-trastuzumab emtansine）
生产厂家：
药品简介
近日，抗体偶联药物Kadcyla（trastuzumab emtansine，T-DM1）获欧盟批准上市。Kadcyla是一种HER2靶向性疗法，是一种由罗氏曲妥珠单抗与ImmunoGen公司DM1细胞毒制剂相偶联的药物，具有2种抗癌属性：曲妥珠单抗的HER2抑制和DM1的细胞毒性。曲妥珠单抗和DM1之间采用一种稳定的连接子（linkers）偶联，将DM1递送至HER2阳性乳腺癌细胞。
批准日期：2013年11月2日；公司：罗氏（Roche）
KADCYLA（曲妥珠单抗[ado-trastuzumab emtansine]）用于注射，用于静脉内使用
作用机制
Ado-trastuzumab emtansine是HER2靶向的抗体-药物偶联物。 抗体是人源化抗HER2 IgG1，曲妥珠单抗。 小分子细胞毒素DM1是微管抑制剂。在结合HER2受体的亚结构域IV后，曲妥珠单抗美登素经历受体介导的内化和随后的溶酶体降解，导致含有DM1的细胞毒性分解代谢物的细胞内释放。DM1与微管蛋白的结合破坏细胞中的微管网络，其导致细胞周期停滞和凋亡性细胞死亡。 此外，体外研究表明，类似于曲妥珠单抗，阿曲古妥珠单抗美登素抑制HER2受体信号传导，介导抗体依赖性细胞介导的细胞毒性，并抑制过度表达HER2的人乳腺癌细胞中HER2细胞外结构域的脱落
适应症和用法
KADCYLA是HER2靶向抗体和微管抑制剂缀合物，作为单一药剂，用于治疗HER2阳性的转移性乳腺癌患者，所述HER2阳性，转移性乳腺癌先前分别或组合接受曲妥珠单抗和紫杉烷。患者应该有：
接受先前治疗转移性疾病，或
在完成辅助治疗的6个月内或在6个月内发展的疾病复发。
剂量和给药
仅用于静脉输注。不要作为静脉推注或推注给药。不要使用葡萄糖（5％）溶液。
KADCYLA的推荐剂量为3.6mg/kg，作为每3周（21天周期）的静脉内输注，直到疾病进展或不可接受的毒性。不要以大于3.6mg/kg的剂量施用KADCYLA。不要用KADCYLA替代或用曲妥珠单抗替代。
不良事件（输注相关反应，肝毒性，左心室心脏功能障碍，血小板减少，肺部毒性或周围神经病变）的管理可能需要暂时中断，减少剂量或停止治疗KADCYLA。
剂量形式和强度
冻干粉末在一次性小瓶中，每瓶含有100毫克或每瓶160毫克。
禁忌症
没有。
警告和注意事项
肺毒性：在诊断为间质性肺病或肺炎的患者中永久停用KADCYLA。
输液相关反应，超敏反应：监测输液期间和之后的体征和症状。如果发生显着的输注相关反应或超敏反应，则减慢或中断输注并施用适当的医学治疗。永久停止KADCYLA的危及生命的输液相关反应。
出血：在没有已知确定的危险因素的患者中，以及在血小板减少症患者和接受抗凝血和抗血小板治疗的患者中，在临床试验中发生致死性出血。使用这些试剂时要小心，并在医疗上同时使用时考虑额外的监测。
血小板减少：在每次KADCYLA剂量之前监测血小板计数。适当调整剂量修改。
神经毒性：监测体征或症状。对于经历3或4级外周神经病变的患者暂时停止给药。
HER2测试：使用经过FDA批准的实验室进行的测试，证明其熟练。
不良反应
与KADCYLA（n=884名治疗的患者）最常见的不良药物反应（频率> 25％）是疲劳，恶心，肌肉骨骼疼痛，出血，血小板减少，头痛，转氨酶增加，便秘和鼻出血。
在特定人群中使用
哺乳：建议不要哺乳。
女性和男性的生殖潜力：验证女性在KADCYLA开始之前的怀孕状态。
Kadcyla 100 mg & 160 mg Powder for Concentrate for Solution for Infusion
KADCYLA  is approved to treat HER2-positive breast cancer that has spread to other parts of the body (metastatic breast cancer) after prior treatment with trastuzumab (Herceptin®) and a taxane. Prior treatment could have been for the initial treatment of breast cancer or for the treatment of cancer that had spread to other parts of the body.
KADCYLA (ado-trastuzumab emtansine)
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 Important Safety Information
What is the most important safety information I should know about KADCYLA?
KADCYLA is not the same medicine as trastuzumab (Herceptin).
Liver problems
KADCYLA may cause severe liver problems that can be life-threatening. Symptoms of liver problems may include vomiting, nausea, eating disorder (anorexia), yellowing of the skin (jaundice), stomach pain, dark urine, or itching
Heart problems
KADCYLA may cause heart problems, including those without symptoms (such as reduced heart function) and those with symptoms (such as congestive heart failure). Symptoms may include swelling of the ankles or legs, shortness of breath, cough, rapid weight gain of greater than 5 lb in less than 24 hours, dizziness or loss of consciousness, or irregular heartbeat
Pregnancy
Receiving KADCYLA during pregnancy can result in the death of an unborn baby and birth defects. Birth control should be used while you receive KADCYLA and for 7 months after your last dose of KADCYLA
If you are exposed to KADCYLA during pregnancy or become pregnant within 7 months of your last dose of KADCYLA, contact your healthcare provider right away; you are also encouraged to enroll in the MotHER Pregnancy Registry by calling 1-800-690-67201-800-690-6720 or visiting http://www.motherpregnancyregistry.com/
You are also encouraged to report exposure to KADCYLA during pregnancy, or if you become pregnant within 7 months of your last dose to Genentech by calling 1-888-835-25551-888-835-2555
If you are a mother who is breastfeeding, you should talk with your doctor about either stopping breastfeeding or stopping KADCYLA
Contact your doctor right away if you experience symptoms associated with these side effects.
What are the additional possible serious side effects of KADCYLA?
Not all people have serious side effects; however, side effects with KADCYLA treatment are common. It is important to know what side effects may happen and what symptoms you should watch for.
Lung problems
KADCYLA may cause lung problems, including inflammation of the lung tissue, which can be life-threatening. Signs of lung problems may include trouble breathing, cough, tiredness, and fluid in the lungs
Infusion-related reactions
Symptoms of an infusion-related reaction may include one or more of the following: the skin getting hot or red (flushing), chills, fever, trouble breathing, low blood pressure, wheezing, tightening of the muscles in the chest around the airways, or a fast heartbeat. Your doctor will monitor you for infusion-related reactions
Serious bleeding
KADCYLA can cause life-threatening bleeding. Taking KADCYLA with other medications used to thin your blood (antiplatelet) or prevent blood clots (anticoagulation) can increase your risk of bleeding. Your doctor should provide additional monitoring if you are taking one of these other drugs while on KADCYLA. Life-threatening bleeding may also happen with KADCYLA, even when blood thinners are not also being taken
Low platelet count
Low platelet count may happen during treatment with KADCYLA. Platelets help your blood to clot. Signs of low platelets may include easy bruising, bleeding, and prolonged bleeding from cuts. In mild cases there may not be any symptoms
Nerve damage
Symptoms may include numbness and tingling, burning or sharp pain, sensitivity to touch, lack of coordination, muscle weakness, or loss of muscle function
Skin reactions around the infusion site
KADCYLA may leak from the vein or needle and cause reactions such as redness, tenderness, skin irritation, or pain or swelling at the infusion site. If this happens, it is more likely to happen within 24 hours of the infusion
How will my doctor know if KADCYLA is right for me?
You must have a HER2 test to determine if your cancer is HER2-positive before taking KADCYLA, because benefit has been shown only in patients whose tumors are HER2-positive.
What are the most common side effects of KADCYLA?
The most common severe side effects of KADCYLA are:
Low platelet count
Liver problems
Low levels of red blood cells
Nerve problems
Low levels of potassium in the blood
Tiredness
The most common side effects seen in people taking KADCYLA were:
Tiredness
Nausea
Pain that affects the bones, muscles, ligaments, and tendons
Bleeding
Low platelet count
Headache
Liver problems
Constipation
Nosebleeds
You are encouraged to report side effects to Genentech and the FDA. You may contact Genentech by calling 1-888-835-25551-888-835-2555. You may contact the FDA by visiting www.fda.gov/medwatch or calling 1-800-FDA-10881-800-FDA-1088.