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Imatinib

印度Imatinib

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-03-27 09:59:24

【药品简介】 Imatinib,酪氨酸激酶抑制剂,是一种小分子蛋白激酶抑制剂,它具有阻断一种或多种蛋白激酶的作用。临床用于治疗慢性髓性白血病和恶性胃肠道间质肿瘤。

【适应症状】 Imatinib,处方药。用于治疗费城染色体阳性的慢性髓性白血病(Ph+CML)的慢性期、加速期或急变期;用于治疗难治复发成人费城染色体阳性的急性淋巴细胞白血病(Ph+ALL);不能手术切除和/或发生转移的恶性胃肠道间质肿瘤(GIST)的成人患者。

【 药品别名 】 格列卫 甲磺酸伊马替尼 Imatinib

印度Imatinib(格列卫 甲磺酸伊马替尼 Imatinib)价格,正品图片,治疗胃癌药物, 购买Imatinib请到印度药房官方网站进行购买 【印度药房大全目录】

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【印度Imatinib说明书,怎么吃?】

【作用机制】   
磺酸伊马替尼在体内外均可在细胞水平上抑制Bcr-Abl酪氨酸激酶,能选择性抑制Bcr-Abl阳性细胞系细胞、Ph染色体阳性的慢性粒细胞白血病和急性淋巴细胞白血病病人的新鲜细胞的增殖和诱导其凋亡。此外,甲磺酸伊马替尼还可抑制血小板衍化生...
 
【副作用】 
多数患者在服用甲磺酸伊马替尼期间会出现一些不良反应,但绝大多数属轻到中度。考虑到疾病本身也会产生症状,常难以明确他们的因果关系。临床试验过程中,因药物相关的不良反应而停药者,在α-干扰素治疗失败的慢粒慢性期患者中仅占1%
给药方法】
 治疗应由对恶性肿瘤患者有治疗经验的医师进行。甲磺酸伊马替尼应在进餐时服用,并饮一大杯水,以使胃肠道紊乱的风险降到最小。通常成人每日一次,每次400mg或600mg,以及日服用量800mg即400mg剂量每天2次(在早上及晚上)。儿童和青少年每日一次或分两次服用(早晨和晚上)。不能吞咽药片的患者(包括儿童),可以将药片分散于不含气体的水或苹果汁中(100mg片约用50ml,400mg约用200ml)。应搅拌混悬液,一旦药片崩解完全应立即服用。只要患者持续受益,本品治疗应持续进行。 推荐的起始治疗剂量:400mg/天
 在治疗后未能获得满意疗效,如果没有严重药物不良反应的话,剂量可考虑从400mg/天增加到600mg/天或800mg/天
 格列卫是一种口服片剂,宜在每日最大餐量时服用,并饮一大杯水
 除非患者有吞咽困难的症状,否则不应将药物掰开或压碎。如果出现这种情况,可将药片溶于一杯水或苹果汁中。

Imatinib

【注意事项】
 如治疗过程中出现严重非血液学不良反应(如严重水潴留),宜停药,直到不良反应消失,随后再根据该不良反应的严重程度调整剂量。
 如胆红质升高超过正常范围上限3倍或转氨酶升高超过正常范围上限5倍,宜停药,直到上述指标分别降到正常范围上限的1.5或2.5倍以下。
 加速期或急变期 :如果出现严重中性粒细胞和血小板减少(中性粒细胞<0.5×109/L和/或血小板<10×109/L,建议剂量减少到400 mg/日。如果血细胞持续减少2周,则进一步减少剂量到300 mg/日,如血细胞持续减少4周,宜停药,直到中性粒细胞≥ (greater than or equal to) 1.0×109/L和血小板≥ (greater than or equal to) 20×109/L。再用时剂量为300 mg/日。
 当中性粒细胞<1.0×109/L和/或血小板<50×109/L时宜停药,仅在中性粒细胞≥ (greater than or equal to) 1.5×109/L和血小板≥ (greater than or equal to) 75×109/L时再恢复用药,剂量为400 mg/日,如中性粒细胞或血小板重新减少到上述数值时,再恢复用药时剂量减至300 mg/日。
 尚无18岁以下患者使用甲磺酸伊马替尼治疗的安全性和有效性临床资料。
 有肝功能损害者甲磺酸伊马替尼的血浆浓度可以升高,因此这些患者用本药时要谨慎,目前尚无肝功能损害患者使用甲磺酸伊马替尼的临床资料,无法提出剂量调整的建议。
 已知肌酐清除率可随年龄老化而降低,而年龄对甲磺酸伊马替尼的药代动力学无明显影响,由于尚未在肾功能损害患者中进行过临床试验,故无法提出剂量调整的建议。
 对本药活性物质或任何赋形剂成份过敏者禁用。孕妇及哺乳期妇女用药禁用。

特殊人群中使用
 
妊娠
 
妊娠类别D[见警告和注意事项(5.11)].
 
当给予妊娠妇女时格列卫可能致胎儿危害。在大鼠当在器官形成期给药剂量100 mg/kg(基于体表面积约等于人最大剂量800 mg/day) 甲磺酸伊马替尼是致畸胎。致畸胎效应包括露脑畸形或脑膨出,额骨缺乏/减小和缺乏顶骨。或早期胎鼠再吸收或假死产,非活存幼畜和产后第0和第4天间早期幼畜死亡率证据表明雌性大鼠给予剂量45 mg/kg(基于体表面积约人最大剂量800 mg/day一半)也经受显著植入后丢失。在剂量较高于100 mg/kg,注意到所有动物总胎鼠丢失。在剂量30 mg/kg(人最大剂量800 mg的三分之一)未见胎鼠丢失。
 
在妊娠妇女中无用格列卫适当和对照良好研究,应建议当用格列卫时不要成为妊娠。如妊娠期间使用此药,或服用此药时成为妊娠,应忠告患者对胎儿的潜在危害。
 
哺乳母亲
 
伊马替尼及其活性代谢物被排泄至人乳。根据来自三例哺乳妇女服用格列卫的资料,乳汁:血浆浓度比值对伊马替尼约0.5和对活性代谢物约0.9。
 
考虑伊马替尼和活性代谢物的联合浓度,根据体重哺乳婴儿可能接受高达10%母体治疗剂量。因为哺乳婴儿来自格列卫的潜在严重不良反应,应做出决策是否中断哺乳或终止药物,考虑药物对母亲的重要性。
 
儿童使用
 
在新诊断Ph+慢性期CML儿童和在Ph+ 慢性期CML儿童中干细胞移植后复发或对干扰素-α治疗耐药已证实格列卫的安全性和疗效。没有2岁以下儿童中的资料。在儿童中新诊断Ph+慢性期CML随访有限。
 
如同成年患者,在患儿中口服给药后伊马替尼被迅速吸收,Cmax为2-4 小时。表观口服清除率与成年值(在儿童中11.0 L/hr/平方米相比在成年10.0 L/hr/平方米)相似,半衰期也一样(在儿童中14.8小时相比成年17.1小时)。在儿童中给药260 mg/平方米和340 mg/平方米二者达到成年中400 mg剂量AUC相似。每天1次重复给药后比较第8天AUC相比第1天AUC,在260 mg/平方米和340 mg/平方米剂量水平揭示分别为1.5-和2.2-倍药物积蓄。伊马替尼AUC均数不与剂量增加成正比例。
 
老年人使用
 
在CML临床研究中,约20%患者年龄大于65岁。新诊断CML患者研究中,6%患者年龄大于65岁。除了水肿较高频数外,大于65岁患者与较年轻患者比较安全性谱形未观察到差异[见警告和注意事项(5.1)]。老年和较年轻患者格列卫疗效相似。
 
在不可切除或转移GIST研究中,16%患者年龄大于65岁。年龄大于65岁患者与较年轻患者比较,未注意到安全性和疗效谱形明显差别,但患者数量小不允许正式分析。
 
在辅助GIST研究中,221例患者(31%)年龄大于65岁。年龄大于65岁患者与较年轻患者比较,除了水肿频数较高,未观察到安全性和疗效谱形差别。老年和较年轻患者格列卫疗效相似。

Imatinib英文说明

Imatinib mesylate uses

Imatinib mesylate is used in the treatment of blood cancer (chronic myeloid leukaemia), Blood cancer (Acute lymphocytic leukemia) and gastrointestinal stromal tumour.

How imatinib mesylate works

Imatinib mesylate is an anti-cancer medication. A protein enzyme, bcr-abl tyrosine kinase, responsible for the growth of abnormal proliferation of cancer cells. This medicine inhibits the proliferation and induces apoptosis (planned cell death) in bcr-abl positive cells (cancer cells). This is how it works to stop or slow the spread of cancer.

Common side effects of imatinib mesylate

Nausea, Rash, Vomiting, Musculoskeletal (bone, muscle or joint) pain, Edema (swelling), Abdominal pain, Fatigue, Diarrhea, Muscle cramp

Imatinib

生物活性

产品描述

matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM).

靶点活性

c-Kit,100 nM (cell free)

PDGFR,100 nM (cell free)

v-Abl,600nM

体外活性

Imatinib (STI 571) inhibited c-kit autophosphorylation, activation of mitogen-activated protein (MAP) kinase, and activation of Akt without altering total protein levels of c-kit, MAP kinase, or Akt. The concentration that produced 50% inhibition for these effects was approximately 100 nmol/L. STI 571 also significantly decreased SLF-dependent growth of M-07e cells in a dose-dependent manner and blocked the antiapoptotic activity of SLF [1]. Imatinib mesylate had a more similar effect on Bcr/Abl- and c-Kit–dependent proliferation, with an IC50 of 19 nM in R10(-) cells and 82 nM in MO7e cells growing in the presence of SCF (KL, Kit ligand), respectively [2]. STI571 inhibited tyrosine phosphorylation and cell growth of Ba/F3 cells expressing BCR/ABL, TEL/ABL, TEL/PDGFbetaR, and TEL/ARG with an IC(50) of approximately 0.5 microM in each case, but it had no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by TEL/JAK2 [3].

体内活性

Imatinib (25 mg/kg/day, p.o.) significantly reduced the endometriosis score compared to normal saline. It significantly decreased the ovarian follicle number compared to normal saline. The CD117 staining score of rats administered imatinib was significantly lower than that of the rats received normal saline [4]. After intraperitoneal injection of STI571, it has 80%, 40% and 78% growth inhibition of SCLC6, SCLC61, and SCLC108 tumors, respectively, without any significant inhibition of SCLC74 tumor growth [5].

激酶实验

PDGF receptor kinase activity: PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-33P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.

细胞实验

M-07e cells were grown in serum-free RPMI 1640 at 37°C for approximately 18 hours before they were incubated for 90 minutes in the presence of various concentrations of STI 571. The cells were then pelleted and resuspended in 1 mL RPMI 1640. STI 571 was added to each tube to achieve the same concentration used during the 90 minutes of preincubation. The cells were then incubated with inhibitor and growth factor (SLF or GM-CSF) for 15 minutes at 37°C. Subsequently, the cell pellets were lysed with 100 to 250 μL of protein lysis buffer (50 mmol/L Tris, 150 mmol/L sodium chloride, 1% NP-40, and 0.25% deoxycholate, with addition of the inhibitors aprotinin, leupeptin, pepstatin, phenylmethyl sulfonyl fluoride, and sodium orthovanadate). Western immunoblot analysis was performed as previously described.41Experiments with HMC-1 cells were performed in the same way except that neither SLF nor GM-CSF was added [1].

细胞系: BON-1 cells and NCI-H727 cells

动物实验

Swiss mice (nu/nu, female), weighing 30 g, 6 – 8 weeks old, were bred in the animal facilities, maintained under specific pathogen-free conditions with artificial lighting (12 hr light/12 hr dark cycle) and fed a regular diet and water ad libitum. For therapeutic trials, the tumor-bearing mice were randomly divided into equivalent groups of 5 to 12 animals and mice were treated as soon as the xenografted tumors reached a diameter of 5 mm (or a tumor volume of approximately 60 mm^3). Four different human tumors were used: the SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers. STI571 was administered at a total dosage of 70 or 100 mg/kg per day in 1 or 2 intraperitoneal injections, with or without etoposide plus ifosfamide or topotecan. STI571 was diluted in 150 l of H2O and administered on different days, as indicated. Etoposide and ifosfamide were diluted in 200 l of 0.9% sodium chloride, and topotecan was diluted in 150 l of 0.9% sodium chloride. The control group received injections according to the same schedule as experimentally treated mice. All mice were weighed once weekly. Tumor growth was monitored by measuring 2 perpendicular diameters with calipers. Tumor volume (V) and the relative tumor volume (RTV) were calculated as: V = a^2 × b/2, where a is the width (large diameter) and b the length (small diameter) of the tumor in millimeters, and RTV = Vx/Vi, where Vx is the mean tumor volume in cubic millimeters at any given time and Vi is the mean initial tumor volume in cubic millimeters at the start of treatment. Mice were ethically sacrificed when the tumor volume reached 2,500 mm^3 [5].

动物模型:SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).

化学信息

分子量

493.60

分子式

C29H31N7O

CAS

152459-95-5

溶解度

DMSO: 66.9 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

  1 mg 5 mg 10 mg
1 mM 2.026 ml 10.13 ml 20.259 ml
5 mM 0.405 ml 2.026 ml 4.052 ml
10 mM 0.203 ml 1.013 ml 2.026 ml
50 mM 0.041 ml 0.203 ml 0.405 ml


参考文献
 
1. Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32.
2. Wolff NC, et al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood. 2005 May 15;105(10):3995-4003. Epub 2005 Jan 18.
3. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8
4. Yildiz C, et al. Effect of imatinib on growth of experimental endometriosis in rats. Eur J Obstet Gynecol Reprod Biol. 2016 Feb;197:159-63.
5. Decaudin D, et al. In vivo efficacy of STI571 in xenografted human small cell lung cancer alone or combined with chemotherapy. Int J Cancer. 2005 Feb 20;113(5):849-56.
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