英文药名：Tasigna Capsules（Nilotinib Hydrochloride Hydrate） 中文药名：盐酸盐尼洛替尼胶囊 生产厂家：日本诺华制药 タシグナカプセル50mg／タシグナカプセル150mg／タシグナカプセル200mg 药物分类名称 抗肿瘤药（酪氨酸激酶抑制剂） 批准日期：2011年3月 商標名 Tasigna Capsules 構造式 一般名 ニロチニブ塩酸塩水和物（Nilotinib Hydrochloride Hydrate） 化学名 4-Methyl-N-［3-（4-methyl-1H-imidazol-1-yl）-5-（trifluoromethyl）phenyl］-3-｛［4-（pyridin-3-yl）pyrimidin-2-yl］amino｝benzamide monohydrochloride monohydrate 分子式 C28H22F3N7O・HCl・H2O 分子量 583.99 性状 白色至黄色黄色白色或绿黄色白色粉末。 它微溶于甲醇或乙醇，极易溶于水。 分布系数 0.08（1-辛醇/0.1mol/L盐酸） 处理注意事项 避免在高温高湿下储存。 药效药理 1. 抗肿瘤作用 (1) 抑制表达Bcr-Abl的白血病细胞系的细胞增殖 在体外细胞培养系统中，尼罗替尼抑制人白血病细胞系和BCR-ABL基因和表达的鼠骨髓细胞系的细胞增殖。 此外，在表达伊马替尼耐药性Bcr-Abl突变体的33只小鼠Ba/F3细胞系中，抑制了32种细胞增殖。 (2) 对Bcr-Abl依赖性白血病动物模型的作用 尼罗替尼抑制静脉移植BCR-ABL转基因细胞的免疫缺陷小鼠的肿瘤生长。 2. 作用机序 尼洛替尼通过抑制Bcr-Abl酪氨酸激酶竞争性地拮抗三磷酸腺苷（ATP）并诱导Bcr-Abl表达细胞中的细胞死亡。 尼罗替尼不仅抑制Bcr-Abl，而且抑制干细胞因子（SCF）受体的c-kit和血小板衍生生长因子（PDGF）受体酪氨酸激酶，但是选择性地作用于Bcr-Abl而不是伊马替尼到。 此外，尼罗替尼可以通过疏水相互作用与伊马替尼耐药的Bcr-Abl突变体结合，并且还抑制许多伊马替尼耐药的Bcr-Abl突变体。 适应病症 慢性或过渡性慢性粒细胞白血病 用法与用量 通常，对于成年人，每天一次400mg一次，因为尼罗替尼在餐前1小时或更多餐后服用2小时，每天两次，每12小时一次口服。 然而，在初期慢性期的慢性骨髓性白血病的情况下，单剂量为300mg。 此外，根据患者的状况进行体重减轻。 包装规格 **胶囊 50mg：20粒（PTP） 150mg：20粒（PTP），120粒（PTP） 200mg：20粒胶囊（PTP），120粒胶囊（PTP） 制造销售 诺华制药公司 完整资料附件：http://www.info.pmda.go.jp/go/pack/4291021M1020_1_23/ Tasigna(nilotinib Capsules) WARNING QT PROLONGATION AND SUDDEN DEATHS •Tasigna prolongs the QT interval. Prior to Tasigna administration and periodically, monitor for hypokalemia or hypomagnesemia and correct deficiencies (see WARNINGS AND PRECAUTIONS). Obtain ECGs to monitor the QTc at baseline, seven days after initiation, and periodically thereafter, and follow any dose adjustments. •Sudden deaths have been reported in patients receiving nilotinib (see WARNINGS AND PRECAUTIONS). Do not administer Tasigna to patients with hypokalemia, hypomagnesemia, or long QT syndrome (see CONTRAINDICATIONS and WARNINGS AND PRECAUTIONS). •Avoid use of concomitant drugs known to prolong the QT interval and strong CYP3A4 inhibitors. •Patients should avoid food 2 hours before and 1 hour after taking dose (see WARNINGS AND PRECAUTIONS). DRUG DESCRIPTION Tasigna (nilotinib) belongs to a pharmacologic class of drugs known as kinase inhibitors. Nilotinib drug substance, a monohydrate monohydrochloride, is a white to slightly yellowish to slightly greenish yellow powder with the anhydrous molecular formula and weight, respectively, of C28H22F3N7O•HCl• H2O and 584. The solubility of nilotinib in aqueous solutions decreases with increasing pH. Nilotinib is notoptically active. The pKa1 was determined to be 2.1; pKa2 was estimated to be 5.4. The chemical name of nilotinib is 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide, monohydrochloride, monohydrate. Its structure is shown below: Tasigna (nilotinib) Capsules, For Oral Use, contain 150 mg or 200 mg nilotinib base, anhydrous (as hydrochloride, monohydrate) with the following inactive ingredients: colloidal silicon dioxide, crospovidone, lactose monohydrate, magnesium stearate and polyoxamer 188. The capsules contain gelatin, iron oxide (red), iron oxide (yellow), iron oxide (black) and titanium dioxide. What are the possible side effects of nilotinib (Tasigna)? Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using nilotinib and call your doctor at once if you have a serious side effect such as: •feeling like you might pass out, fast or pounding heartbeat, seizure (convulsions); •pale skin, weakness, feeling light-headed, rapid heart rate, trouble concentrating; •easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), purple or red pinpoint spots under your skin; •fever, chills, body. Read All Potential Side Effects and See Pictures of Tasigna Capsules » What are the precautions when taking nilotinib capsules (Tasigna Capsules)? Before taking nilotinib, tell your doctor or pharmacist if you are allergic to it; or to lactose/galactose; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details. Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, pancreatitis. Nilotinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that require immediate medical attention. The risk of QT prolongation may be increased if you have certain medical conditions or are taking。