英文药名：Tafinlar（Dabrafenib Mesilate Capsules）

中文药名：达拉菲尼胶囊

生产厂家：诺华制药

タフィンラーカプセル50mg／タフィンラーカプセル75mg

治疗类别名称
抗肿瘤药
BRAF抑制剂
商標名
Tafinlar Capsules
構造式

一般名
ダブラフェニブメシル酸塩（Dabrafenib Mesilate）
化学名
N-｛3-［5-（2-Aminopyrimidin-4-yl）-2-（1,1-dimethylethyl）-1,3-thiazol-4-yl］-2-fluorophenyl｝-2,6-difluorobenzenesulfonamide monomethanesulfonate
分子式
C23H20F3N5O2S2・CH4O3S
分子量
615.67
性状
白色到浅黄白色粉末。
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) Daburafenibu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，抑制来自人恶性黑色素瘤表达突变的WM-115细胞系YULAC和YUSIT1）和BRAF V600D的生长。
2) Daburafenibu，与Trametinib一个MEK1和MEK2抑制剂，针对UACC-257的增殖抑制效果的组合，SK-MEL-1，COLO-829细胞系等进行比较，以每种药物单独处理增强。
(2) 体内（In vivo）
Daburafenibu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Daburafenibu和Trametinib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
Daburafenibu抑制BRAF突变（V600E，V600K和V600D）的激酶活性。此外，Daburafenibu与A375P F11细胞系移植小鼠的肿瘤组织中抑制ERK的下游RAF信号传导途径的磷酸化。
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
成人：每日口服二次（为150毫克），空腹口服给药。此外，根据该状态的患者用药。
包装规格
胶囊
50毫克*28粒（塑料瓶）
75毫克*28粒（塑料瓶）

制造商
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/4291046M1020_1_02/
Tafinlar Capsules（Dabrafenib mesilate）
Tafinlar Capsules 50mg（タフィンラーカプセル50mg） 
Brand name : Tafinlar Capsules 50mg
　Active ingredient: Dabrafenib mesilate
　Dosage form: dark red opaque capsule, major axis: 18.0 mm, minor axis: 6.4 mm
　Print on wrapping:
Tafinlar Capsules 75mg（タフィンラーカプセル75mg） 
Brand name : Tafinlar Capsules 75mg
　Active ingredient: Dabrafenib mesilate
　Dosage form: dark reddish white opaque capsule, major axis: 19.4 mm, minor axis: 6.9 mm
　Print on wrapping: 
Effects of this medicine
This medicine suppresses cancer cell growth by inhibiting MAPK pathway which is essential to cancer cell growth via inhibiting mutated BRAF kinase.
It is usually used to treat unresectable malignant melanoma with BRAF gene mutations.
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, 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 (150 mg as dabrafenib) at a time on an empty stomach, twice a day. The dosage may be decreased according to the symptoms. Strictly follow the instructions.
•Avoid taking the medicine between 1 hour before and 2 hours after meals, since it may become difficult to be absorbed if taken after meals, resulting in insufficient efficacy.
•If you miss a dose and have more than 6 hours until the next dose, take the missed dose as soon as possible. If the next dose is within 6 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
•If women of reproductive potential and their partners should use effective contraception during and certain time period after taking this medicine, since toxicity has been reported in animal studies.
Possible adverse reactions to this medicine
The most commonly reported adverse reactions include fever, chills, fatigue, edema of limbs, hyperkeratosis (hardening and thickening of the skin), skin papilloma, alopecia and joint pain. 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.
•bumps or ulcers on the skin covered with erosion or scabs, new malignant tumor [squamous cell carcinoma, malignant tumor (secondary cancer)]
•palpitation, shortness of breath, edema [heart disorder]
•general malaise, loss of appetite, nausea, jaundice [liver dysfunction]
•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 away from direct sunlight, heat and moisture.
•Discard the remainder. Do not store them. Ask your pharmacy 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.