英文药名：SUTENT Capsule（Sunitinib Malate） 中文药名：苹果酸舒尼替尼胶囊 生产厂家：辉瑞公司 スーテントカプセル12.5mg 药物分类名称 抗肿瘤剂/激酶抑制剂 批准日期：2008年6月 商標名 SUTENT Capsule 一般名 スニチニブリンゴ酸塩（Sunitinib Malate） 化学名 N-［2-（Diethylamino）ethyl］-5-［（Z）-（5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene）methyl］-2,4-dimethyl-1H-pyrrole-3-carboxamide mono［（2S）-2-hydroxysuccinate］ 分子式 C22H27FN4O2・C4H6O5 分子量 532.56 構造式 性状 苹果酸舒尼替尼是一种黄色至近似颜色的粉末。 微溶于二甲基亚砜，微溶于N，N-二甲基甲酰胺，难溶于水或甲醇，极难溶于乙醇（99.5）。 溶于0.1mol/L盐酸试剂溶液。 分配系数（log D） 2.7（pH 7.4,1-辛醇/水） 药效药理 1.抗肿瘤作用 显示肿瘤生长抑制的效果，肿瘤在人类肿瘤异种移植物，小鼠同基因白血病，转基因小鼠和化学致癌性啮齿动物肿瘤模型中的消退。 2.血管生成抑制作用 体外抑制血管内皮细胞的VEGF增殖和血管内皮细胞的萌发。 另外，在移植了人类肿瘤异种移植裸鼠和人类新生儿包皮的SCID小鼠中，移植部位的血管生成受到抑制。 3. 作用机序 体外研究表明，血小板源性生长因子受体（PDGFR - α和PDGFR - β），血管内皮生长因子受体（VEGFR - 1，VEGFR - 2和VEGFR - 3），干细胞因子受体 抑制fms样酪氨酸激酶3（FLT3），集落刺激因子1受体（CSF-1R）和神经胶质细胞衍生的神经营养因子受体（RET）的受体酪氨酸激酶活性。 抑制PDGFR-β，VEGFR-2，KIT和FLT3的磷酸化也在体内肿瘤中观察到。 4.代谢产物的药理作用 在体外试验中，该药物和无代谢体系或细胞系统中用于磷酸化VEGFR-2，PDGFR-β和KIT的主要代谢物（N-去乙基化）的Ki值或IC50值为3至13nmol/L和2〜20 nmol/L，表达VEGFR-2，PDGFR-α或PDGFR-β的细胞分别为4〜69 nmol/L和20〜100 nmol/L。 适应病症 伊马替尼耐胃肠道间质瘤 肾可切除或转移性肾细胞癌 胰腺神经内分泌肿瘤 用法与用量 伊马替尼耐胃肠道间质瘤，根治性可切除或转移性肾细胞癌 成年人，每天一次口服50mg，口服舒尼替尼4周，然后停药2周。 另外，根据患者的状况来减轻体重。 胰腺神经内分泌肿瘤 成人，舒尼替尼每天口服一次37.5毫克。 根据病人的情况，可适当增加或减少，但可每天增加至50毫克。 包装 胶囊 12.5毫克：14粒×4片（PTP） 制造商 辉瑞公司 注：以上中文资料不够完整，使用者以原处方资料为准。 完整说明书附件：http://www.info.pmda.go.jp/go/pack/4291018M1029_2_10/ SUTENT Capsule（Sunitinib Malate）スーテントカプセル12.5mg Brand name : SUTENT Capsule 12.5mg 　Active ingredient: Sunitinib malate 　Dosage form: capsule with deep red-brown cap and body, φ5.3 mm, length 14.3 mm 　Print on wrapping: スーテント12.5mg, SUTNET12.5mg, STN12.5 Effects of this medicine This medicine has an anti-tumor effect by suppressing the receptor associated with tumor proliferation and vascularization. Usually, used for treatment of imatinib-resistant gastrointestinal stromal tumor, radically unresectable or metastatic renal cell carcinoma and pancreatic neuroendocrine tumors. Before using this medicine, be sure to tell your doctor and pharmacist •If you have previously experienced any allergic reaction (itch, rash etc.) to any medicine. If you have: heart problems such as heart failure. •If you are pregnant, breastfeeding or possibly pregnant. •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>> •For imatinib-resistant gastrointestinal stromal tumor and radically unresectable or metastatic renal cell carcinoma: in general, for adults, take 4 capsules (50 mg of sunitinib) once a day for consecutive 4 weeks. Then, discontinue taking for 2 weeks. This treatment course is repeated. The dosage should be adjusted according to your symptoms. For pancreatic neuroendocrine tumors: in general, for adults, take 3 capsules (37.5 mg of sunitinib) once a day. The dosage should be adjusted according to your symptoms. However, the daily dosage is up to 4 capsules(50 mg) once a day. Strictly follow the instructions in either case. •If you missed a dose, skip the missed dose and continue your regular dosing schedule. You should never take two doses at one time. •If you accidentally took more than your prescribed dose, consult with your doctor or pharmacist. •Do not stop taking the medicine unless your doctor instructs you to do so. Precautions while taking this medicine •This medicine may cause dizziness, drowsiness or loss of consciousness. Be very careful when working at heights, driving a car or operating machinery. •Avoid taking food containing St. John's wort (a kind of herb) with the medicine, because the effect of the medicine may be decreased. •Avoid drinking grapefruit juice with the medicine, because the effect of the medicine may be increased. Possible adverse reactions to this medicine The most commonly reported adverse reactions include skin discoloration, hand-and-foot syndrome (tingling, hot flash, swelling), loss of appetite, fatigue, diarrhea, anemia, hypertension and abnormal liver function. 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. •anemia, fever, bleeding tendency [myelosuppression] •throat pain, rash, bacterial infection  [infections] •nose bleeding, subcutaneous bleeding, oral bleeding [bleeding] •dullness, palpitation, fainting  [heart failure, arrhythmia] •sweating, dullness, impotent feeling [thyroid dysfunction] 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. If you dispose of unused medicines, seek advice of your pharmacist about proper disposal of drugs Pfizer Pharmaceuticals Inc.Internal Revised: 8/2012 ------------------------------------------------- 产地国家：日本 原产地英文商品名: SUTENT(スーテント)12.5mg/cap 56caps/box 原产地英文药品名: SUNITINIB MALATE 中文参考商品译名: 索坦胶囊(スーテント)12.5毫克/胶囊 56胶囊/盒 中文参考药品译名: 苹果酸舒尼替尼 生产厂家中文参考译名: Pfizer 生产厂家英文名: Pfizer