英文药名: Gleevec(Imatinib Mesylate) 中文药名: 格列卫（甲磺酸伊马替尼胶囊） 生产厂家: Novartis 给药说明 甲磺酸伊马替尼（Imatinib Mesylate）由瑞士诺华公司（Novartis）发明研制的新型抗癌药物，是一种选择性酪氨酸激酶抑制剂（A tyrosine kinase inhibitor），属苯胺喹唑啉类化合物。该药物通过抑制酪氨酸激酶来有效治疗胃肠基质肿瘤（Gastrointestinal Stromal Tumor，GIST）和血癌，即慢性骨髓性白血病（Chronic Myelogenous Leukemia，CML)。 药理作用 本品为苯氨嘧啶的衍生物，属新型酪氨酸激酶抑制剂。约95%的慢性粒细胞白血病(chronic myelocytic leukemia，CML)患者均有ph1染色体阳性，即9号染色体的原癌基因ABL异位到22号染色体的一段称为断裂点成簇区(breakpoint clustering region，BCR)的癌基因上，两种基因重组在一起，产生融合蛋白p-210，与正常的C-ABL蛋白p-150相比，p-210具有较高的酪氨酸激酶活性，可刺激白细胞增殖，导致白血病。本品在体内外均可强烈抑制ABL酪氨酸激酶的活性，特异性地抑制ABL的表达和BCR-ABL细胞的增殖，从而可用于治疗CML。此外，本品尚可抑制血小板衍化生长因子(platelet-derived growth factor，PDGF)和干细胞因子(stemcellfactor，SCF)受体的酪氨酸激酶，并可抑制PDGF和SCF介导的生化反应，但不影响其他刺激因子(如表皮生长因子等)的信号传导。 药动学 本品口服易于吸收，2～4h后血药浓度达峰值，口服生物利用度为98%，蛋白结合率为95%。临床前研究表明，本品不易透过血-脑脊液屏障。药物主要在肝脏被代谢为具有药理活性的代谢物(N-去甲基哌嗪衍生物)，原形药和代谢物的半衰期分别为18h、40h。口服本品后7天内，约81%排出体外(68%经粪便排泄，13%经尿液排出)，其中约25%为药物原形(尿中占5%，粪便中占20%)。 适应证 用于治疗各期慢性髓细胞白血病(CML)。也用于治疗CD117阳性的胃肠道间质细胞瘤(GIST)。 禁忌证 对本品过敏者禁用。 1.肝功能不全者慎用。 2.严重心力衰竭者慎用。 3.动物实验表明本品有致畸性，尚缺乏孕妇的用药资料，孕妇慎用。 4.可大量分泌人动物乳汁中，在人乳汁中的分布情况尚不清楚，哺乳期妇女慎用。 5.骨髓抑制者慎用。 6.病毒或细菌感染患者慎用。 7.胃肠功能紊乱者慎用。 注意事项 1.治疗前应检查肝功能(包括氨基转移酶、血胆红素和碱性磷酸酶)，以后可每月复查1次。 2.治疗的第1个月宜每周检查血常规，第2个月每2周检查1次。 3.建议定期监测体重。 不良反应 1.血液系统：可见中性粒细胞减少(14%)、血小板减少(14%)和贫血(11%)。中性粒细胞减少性发热、全血细胞减少也常见。 2.代谢内分泌系统：常见食欲缺乏，少见食欲增加、脱水、血尿酸及血钾升高或血钾及血钠降低。 3.神经精神系统：常见头痛(11%)、头晕、味觉障碍、失眠，少见出血性卒中、晕厥、周围神经病变、感觉减退、嗜睡、偏头痛及抑郁。 4.眼、耳：常见结膜炎、泪多，少见眼刺激症状、视力模糊、结膜出血、眼干、眶周浮肿及耳和迷路异常。 5.心血管系统：少见心力衰竭、肺水肿、心动过速、高血压、低血压、皮肤潮红、四肢发冷及血肿。 6.呼吸系统：常见胸水、鼻衄，少见呼吸困难、咳嗽。 7.消化系统：常见恶心(56%)、呕吐(33%)、腹泻(24%)、消化不良(12%)、腹痛、腹胀、便秘、口干，少见胃肠出血、腹水、胃溃疡、胃炎、胃食管反流、口腔溃疡、氨基转移酶及血胆红素升高等肝功能异常。 8.皮肤：常见全身浮肿(30%)、各类皮炎及皮疹(约25%)、皮肤瘙痒、红皮症、皮肤干燥、脱发、盗汗。少见淤斑、多汗、荨麻疹、指甲断裂、光过敏反应、紫癜。 9.肌肉骨骼系统：可有肌肉痉挛(33%)、关节肿胀及疼痛(25%)，少见坐骨神经痛。 10.泌尿生殖系统：少见血肌酐升高、肾衰竭、男性乳房女性化、乳房肿大、阴囊水肿。 11.其他：常见水潴留(10%)、发热、疲劳乏力、畏寒和体重增加。少见全身不适、出血、体重减轻、败血症、肺炎、疱疹病毒感染等。 用法用量 CML急变期和加速期：口服，推荐开始剂量为每次600mg，1次/d，用药后如病情继续发展(治疗至少3个月后尚没有获得满意的疗效)，且患者没有出现严重不良反应时，可增加至每次400mg，2次/d。出现血液学不良反应，当中性粒细胞计数(ANC)少于0.5×109/L或血小板计数少于10×109/L时，建议减量至每天400mg。如血细胞减少持续2周，则应进一步减量至每天300mg；如血细胞减少持续4周，应停止治疗，直到ANC高于1.0×109/L、血小板计数高于20×109/L后，再恢复用药。干扰素治疗失败的CML慢性期：口服，开始剂量为每次400mg，1次/d，用药后如病情继续发展且患者没有出现严重不良反应时，可增加至每天600mg。当ANC少于1.0×109/L、血小板计数少于50×109/L时应停药；只有当ANC高于1.5×109/L、血小板计数高于75×109/L后，才能恢复用药，剂量为每天400mg，当ANC或血小板计数再次降低时，以后恢复用药，剂量应减至每天300mg。 FDA Approves Updated Indication for Gleevec New Labeling Extends Treatment to 36 Months for Certain GIST Patients After Surgery On Jan. 31, the FDA approved a new indication for Gleevec (imatinib mesylate, Novartis) for use in certain adult patients following surgical removal of KIT (CD117)-positive gastrointestinal stromal tumors (GIST). The new labeling recommends 36 months of treatment with Gleevec after surgery in adult patients with KIT-positive GIST who meet the risk for recurrence inclusion criteria of the pivotal trial. The 36-month treatment regimen was shown to improve recurrence-free survival (RFS) and overall survival (OS) in patients with KIT-positive GIST compared with 12 months of treatment. The new approval is based on data from an international, multicenter, open-label Phase III clinical trial (SSG XVIII) conducted by the Scandinavian Sarcoma Group and the Sarcoma Group of the Arbeitsgemeinschaft Internistische Onkologie. Gleevec manufacturer Novartis provided funding for the study. The primary end point of the study was to compare, within the first five years, RFS in patients with a greater than 50% estimated risk for GIST recurrence following diagnosis and treatment with adjuvant Gleevec for either 12 or 36 months. Results of the study revealed that RFS was longer for patients assigned to receive 36 months of Gleevec after surgery compared with those who received 12 months of treatment, for a 54% reduction in risk for GIST recurrence (hazard ratio [HR], 0.46; 95% confidence interval [CI], 0.32-0.65; P<0.0001). Additionally, OS was longer in the 36-month treatment group, which resulted in a 55% reduction in the risk for death (HR, 0.45; 95% CI, 0.22-0.89; P=0.0187). Gleevec was originally granted accelerated approval for the treatment of advanced or metastatic GIST in 2002. In 2008, Gleevec was granted accelerated approval for adjuvant use for the treatment of patients with GIST who had had potentially curative resection (surgical removal) of GIST, but who had an increased risk for recurrence. Approval for the metastatic GIST indication also was granted in 2008. “The development of Gleevec over the past decade highlights the need to further study drugs after approval to truly characterize their benefits,” said Richard Pazdur, MD, director of the Office of Hematology and Oncology Products in the FDA’s Center for Drug Evaluation and Research, in a press release. “Although originally approved in the metastatic disease setting, this subsequent trial has demonstrated that longer use of Gleevec can prolong patients’ lives in earlier disease settings.” GIST is a rare form of cancer that originates in cells found in the wall of the gastrointestinal tract. These cells, known as interstitial cells of Cajal, are part of the autonomic nervous system, which regulates body processes such as food digestion. The major cause of GIST is an abnormal form of the protein KIT, which causes cells to grow uncontrollably and become cancerous. Gleevec is indicated for the treatment of patients with KIT-positive GIST that are cancerous, cannot be surgically removed and/or have spread to other parts of the body. The drug also is approved for use after surgery in patients who have had KIT-positive GIST completely removed. Additionally, Gleevec is approved for the treatment of other cancers; it was first approved by the FDA in 2001 to treat patients with advanced Philadelphia chromosome-positive chronic myeloid leukemia, a blood and bone marrow disease linked to a genetic abnormality. http://www.kegg.jp/medicus-bin/japic_med?japic_code=00062784 http://www.info.pmda.go.jp/go/pack/4291011F1109_1_03/4291011F1109_1_03?view=body --------------------------------------------- 注：以下产品不同规格和不同价格，购买以在线咨询为准！ --------------------------------------------- 产地国家: 瑞士 原产地英文商品名: GLIVEC 100mg/cap 120caps/box 原产地英文药品名: IMATINIB MESYLATE 中文参考商品译名: 格列卫 100毫克/胶囊 120胶囊/盒 中文参考药品译名: 甲磺酸伊马替尼 生产厂家中文参考译名: 诺华制药 生产厂家英文名: Novartis --------------------------------------------- 产地国家: 日本 原产地英文商品名: IMATINIB（イマチニブ錠）100mg/TABLETS 20TABLETS/box 原产地英文药品名: IMATINIB MESYLATE 中文参考商品译名: IMATINIB（イマチニブ錠）100毫克/片 20片/盒 中文参考药品译名: 甲磺酸伊马替尼 生产厂家英文名: Nipro Corporation --------------------------------------------- 产地国家: 日本 原产地英文商品名: IMATINIB（イマチニブ錠）100mg/TABLETS 120TABLETS/box 原产地英文药品名: IMATINIB MESYLATE 中文参考商品译名: IMATINIB（イマチニブ錠）100毫克/片 120片/盒 中文参考药品译名: 甲磺酸伊马替尼 生产厂家英文名: Nipro Corporation --------------------------------------------- 产地国家: 日本 原产地英文商品名: IMATINIB（イマチニブ錠）200mg/TABLETS 20TABLETS/box 原产地英文药品名: IMATINIB MESYLATE 中文参考商品译名: IMATINIB（イマチニブ錠）200毫克/片 20片/盒 中文参考药品译名: 甲磺酸伊马替尼 生产厂家英文名: Nipro Corporation --------------------------------------------- 产地国家: 日本 原产地英文商品名: IMATINIB（イマチニブ錠「明治」）100mg/TABLETS 20TABLETS/box 原产地英文药品名: IMATINIB MESYLATE 中文参考商品译名: IMATINIB（イマチニブ錠「明治」）100毫克/片 20片/盒 中文参考药品译名: 甲磺酸伊马替尼 生产厂家英文名: Meiji Seika --------------------------------------------- 产地国家: 日本 原产地英文商品名: IMATINIB（イマチニブ錠「明治」）200mg/TABLETS 20TABLETS/box 原产地英文药品名: IMATINIB MESYLATE 中文参考商品译名: IMATINIB（イマチニブ錠「明治」）200毫克/片 20片/盒 中文参考药品译名: 甲磺酸伊马替尼 生产厂家英文名: Meiji Seika