英文药名：Inlyta Tablets（Axitinib） 中文药名：阿西替尼片 生产厂家：辉瑞公司 スーグラ錠25mg／スーグラ錠50mg 药物分类名称 抗肿瘤剂/激酶抑制剂 批准日期：2012年8月 商標名 Inlyta Tablets 一般名 アキシチニブ（Axitinib） 化学名 N-Methyl-2-（｛3-［（1E）-2-（pyridin-2-yl）ethen-1-yl］-1H-indazol-6-yl｝sulfanyl）benzamide 分子式 C22H18N4OS 分子量 386.47 構造式 性状 阿西替尼是白色至淡黄色粉末。 易溶于N，N-二甲基乙酰胺，几乎不溶于乙醇（99.5）和0.1 mol / L盐酸，难溶于水。 分配系数（log D） 3.5（pH6.5,1-辛醇/水） 药效药理 1.抗肿瘤作用 在移植了来自人肾细胞癌的SN12C细胞株的小鼠中，显示肿瘤生长抑制作用。 2. 作用机序 (1)抑制血管内皮生长因子受体（VEGFR-1，VEGFR-2和VEGFR-3）的磷酸化并抑制下游信号传导。 (2)在用人肿瘤细胞系移植的小鼠中，在给予贝伐单抗时观察到肿瘤的血管内皮细胞数目减少和总血流速度降低。 此外，在施用贝伐单抗时天然发生胰岛细胞肿瘤的RIP-Tag2转基因小鼠中观察到抑制肿瘤中的血管生成。 适应症 肾可切除或转移性肾细胞癌 用法与用量 成人口服5毫克，每日一次，两次作为阿西替尼。 另外，根据患者的情况可以增加或减少，但是一天一次可增加到一天两次10mg。 包装规格 片 1毫克：50片（PTP） 5毫克：10片（PTP 制造和销售（进口） 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/4291027F1029_1_05/ INLYTA®(axitinib)片为治疗一类晚期肾癌患者，用于治疗其他药物治疗无效的晚期肾细胞癌患者。Axitinib是一种新的、主要靶向于酪氨酸激酶（包括VEGFR）、抑制血管生成的小分子抗癌药。肾细胞癌是起源于肾小管上皮细胞的一种肿瘤，Inlyta通过阻断激酶蛋白起到抑制肿块生长和癌症进展。 Inlyta tablets（Axitinib）インライタ錠 Inlyta tablets 1mg（インライタ錠1mg） Brand name : Inlyta tablets 1mg 　Active ingredient: Axitinib 　Dosage form: red tablet, major axis: 8.6 mm, minor axis: 4.3 mm, thickness: 2.8 mm 　Print on wrapping: インライタ1mg, Pfizer 1XNB, インライタ 1 Inlyta Inlyta tablets 5mg（インライタ錠5mg） Brand name : Inlyta tablets 5mg 　Active ingredient: Axitinib 　Dosage form: red tablet, major axis: 7.7 mm, thickness: 3.8 mm 　Print on wrapping: インライタ5mg, Pfizer 5XNB, インライタ 5 Inlyta Effects of this medicine This medicine has an anti-tumor effect inhibiting angiogenesis and suppressing the tumor cell growth and metastasis by selectively inhibiting vascular endothelial growth factor receptors (VEGFR-1, -2, and -3). Usually, used for treatment of radically unresectable or metastatic renal cell carcinoma. 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, 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>> In general, for adults, take 1 tablet (5 mg of the active ingredient) at a time twice a day. The dosage may be adjusted according to the patient's symptoms. However, the daily dosage is up to 2 tablets (10 mg) at a time twice a day. Strictly follow the instructions. If you miss a dose, take the missed dose as soon as possible. However, you should take the missed dose by three hours before the next dosing schedule or 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 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 diarrhea, constipation, vomiting, nausea, abdominal pain, stomatitis, hypertension, dysphonia, cough, loss of appetite, hand-and-foot syndrome (tingling, hot flash, swelling), rash, dry skin, joint pain, fatigue, asthenia, decreased weight, mucosal inflammation, chest pain, dullness, headache, hypothyroidism, dysgeusia, nasal bleeding and edema. 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. headache, fever, sudden increase in blood pressure [hypertension, high blood pressure crisis] decreased sweating, bradycardia, dry skin, sweating, tachycardia [thyroid dysfunction] nasal bleeding, hematuria, black stool [hemorrhage] severe abdominal pain, melena, hematemesis [perforation of the digestive tract, fistula formation] dullness (general), loss of appetite, yellowing of the skin or whites of the eyes [liver 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 Published: 8/2012 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. -------------------------------------------------------- 产地国家: 日本 原产地英文商品名: INLYTA（インライタ錠） 1MG/TAB 50TABS/BOTTLE 原产地英文药品名: AXITINIB 中文参考商品译名: INLYTA（インライタ錠） 1毫克/片 50片/盒 中文参考药品译名: 阿西替尼 生产厂家中文参考译名: 辉瑞日本公司 生产厂家英文名: Pfizer Japan Inc --------------------------------------------------------------- 产地国家: 日本 原产地英文商品名: INLYTA（インライタ錠） 5MG/TAB 10TABS/BOTTLE 原产地英文药品名: AXITINIB 中文参考商品译名: INLYTA（インライタ錠） 5毫克/片 10片/盒 中文参考药品译名: 阿西替尼 生产厂家中文参考译名: 辉瑞日本公司 生产厂家英文名: Pfizer Japan Inc