英文药名：Mekinist Tablets（Trametinib Dimethyl Sulfoxide） 中文药名：曲美替尼/二甲基亚砜片 生产厂家：诺华制药 メキニスト錠0.5mg／メキニスト錠２mg 治疗类别名称 抗肿瘤药 BRAF抑制剂 批准上市日期：2016年6月 商標名 Mekinist Tablets 構造式 一般名 トラメチニブ　ジメチルスルホキシド付加物（Trametinib Dimethyl Sulfoxide） 化学名 N-（3-｛3-Cyclopropyl-5-［（2-fluoro-4-iodophenyl）amino］-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido［4,3-d］pyrimidin-1（2H）-yl｝phenyl）acetamide-（methylsulfinyl）methane（1：1） 分子式 C26H23FIN5O4・C2H6OS 分子量 693.53 性状 白色粉末。 操作注意事项 1.为了避免光和水分，可以存储在原来的容器，将其包围的干燥剂。 2.密封每次使用。 条件批准 1.建立药品风险管理计划的顶部，要正确实施。 2.由于试验病人在日本是非常有限的，上市后，直至有关一定数量的病例数据集成，通过实现对一切案件的使用，结果调查显示，这使得它能够及早发现这种药物的使用患者的背景资料，数据收集这种药物的安全性和有效性，采取必要的措施，正确使用此药。 药效药理 1.抗肿瘤作用 (1) 体外（In vitro） 1) Trametinib是，BRAF V600E来自人恶性黑色素瘤表达突变的细胞系（UACC-257，SK-MEL-1，COLO-829等），BRAF V600K变体表达人恶性黑色素瘤来源的细胞系衍生的（WW165，YUMAC，抑制从表达的突变体的WM-115细胞系的YULAC和YUSIT1）和BRAF V600D恶性黑色素瘤的生长。 2) Trametinib，结合Daburafenibu一个BRAF抑制剂，针对UACC-257的抗增殖活性，SK-MEL-1，COLO-829细胞系或类似物相比单独每种药物治疗进行增强。 (2) 体内（In vivo） Trametinib是表示在皮下植入抑制肿瘤生长的小鼠的BRAF V600E突变体人恶性黑素瘤衍生A375P F11细胞系。此外，通过Trametinib和Daburafenibu的共同给药，肿瘤增殖抑制效果明显增强相比单独给药每种药物作为。 2. 作用机理 Trametinib抑制MEK1和MEK2的活化和激酶活性。此外，Trametinib与A375P F11细胞系的小鼠的肿瘤组织中植入皮下抑制ERK的磷酸化是对MEK的基板。 适应病症 不能手术切除的根治恶性黑色素瘤与BRAF基因突变。 用法与用量 在与Daburafenibu组合，每天一次为2mg作为Trametinib是内服空腹。此外，根据该状态的患者用药。 包装规格 片剂 0.5毫克*7片（塑料瓶） 2毫克*7片（塑料瓶） 生产商 诺华制药有限公司 注：以上中文资料仅供参考，使用以原处方为准（附）：http://www.info.pmda.go.jp/go/pack/4291047F1026_1_02/ Mekinist Tablets（Trametinib dimethyl sulfoxide） Mekinist Tablets 0.5mg（メキニスト錠0.5mg）  Brand name : Mekinist Tablets 0.5mg 　Active ingredient: Trametinib dimethyl sulfoxide 　Dosage form: yellow oval tablet, major axis: 8.9 mm, minor axis: 4.9 mm, thickness: 3.7 mm 　Print on wrapping: Mekinist Tablets 2mg（メキニスト錠2mg）  Brand name : Mekinist Tablets 2mg 　Active ingredient: Trametinib dimethyl sulfoxide 　Dosage form: pale red circular tablet, diameter: 7.5 mm, thickness: 3.7 mm 　Print on wrapping:  Effects of this medicine This medicine suppresses cancer cell growth by inhibiting MEK kinase, which is essential to cancer cell growth. It is usually used to treat unresectable malignant melanoma with BRAF gene mutations in combination with dabrafenib. 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 are 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 1 tablet (2 mg as trametinib) at a time, once a day on an empty stomach. The dosage may be decreased according to the symptoms. Strictly follow the instructions. It is used in combination with dabrafenib. •Avoid taking the medicine between 1 hour before and 2 hours after meal, since it may become difficult to be absorbed if taken after meal, resulting in insufficient efficacy. •If you miss a dose and have more than 12 hours until the next dose, take the missed dose as soon as possible. If the next dose is within 12 hours, 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. Precautions while taking this medicine •Women of reproductive potential should use effective contraception during and certain time period after taking this medicine. Possible adverse reactions to this medicine The most commonly reported adverse reactions include rash, fever, diarrhea, chills, fatigue and edema of limbs. 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. •palpitation, shortness of breath, edema [heart disorder] •general malaise, loss of appetite, nausea, jaundice [liver dysfunction] •fever, dry cough, respiratory distress [interstitial lung disease] •muscle pain of limbs, stiffness, numbness, lassitude, reddish brown urine [rhabdomyolysis] •regional pain, swelling, respiratory distress, cough, sweating [deep vein thrombosis, pulmonary embolism] •headache, temporary consciousness disorder, one-sided paralysis of limbs, difficulty speaking [cerebrovascular disorder] 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 in the refrigerator (2 to 8 degrees Celsius) and do not freeze. Keep away from light. •Store in the original container with the desiccant. Close the cap tightly each time after you take the medicine. •Discard the remainder. Do not store them. Ask the pharmacist or medical institution on how to discard the remainder. Novartis Pharma K.K.Internal Published: 7/2016 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.