您的位置: 印度药房网 > 医药大数据 > 结直肠癌 >
格列卫

印度格列卫

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-07-09 08:44:31

【药品简介】 适应症为-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。

【适应症状】 格列卫,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

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

播放/暂停

印度全球药房排名

【印度格列卫说明书,怎么吃?】

【格列卫作用机制】   

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。

【格列卫注意事项】
 
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。
格列卫

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。


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.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.

注:本站格列卫(格列卫 甲磺酸伊马替尼 Imatinib)药品说明,价格,正品图片均来自于官方,格列卫如何服用请尊医嘱。如需药品请到正规印度药房进行购买
上一篇:瑞格非尼 下一篇:没有了
格列卫相关药品
瑞格非尼
瑞格非尼

处方药。肝细胞肝癌:用于前期使用过索拉菲尼的肝细胞肝癌。转移性结直肠癌:用于治疗既往曾用含氟嘧啶、奥沙利铂、伊立替康...

格列卫
格列卫

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...

格列卫资讯
格列卫印度版本和国内版本的区别
格列卫印度版本和国内版本的区别

格列卫的专利在几年前就已经到期了,现在国内使用最多的像个版本的仿制药,一个是国产,一个是印度版,印度仿制格列卫早在瑞...

印度格列卫的效果
印度格列卫的效果

格列卫,是广泛应用在白血病治疗中的治疗药物,许多 患者为此并不陌生,尤其是慢性粒细胞白血病患者。格列卫有两个版本,一个...

印度格列卫为什么国内没有卖
印度格列卫为什么国内没有卖

印度格列卫尽管是仿制药,但其药效和原研药是相同的,是能够 治疗慢粒白血病的,那为何印度格列卫在国內买不到呢? 那是由于...

印度格列卫的购买渠道
印度格列卫的购买渠道

格列卫是国际公认的治疗慢性粒细胞白血病的一线药物,能有效延长患者的生命。不过,患者需要长期服用,一盒2.5万元左右,价格...

5招辨别印度格列卫真假
5招辨别印度格列卫真假

印度格列卫由印度Natco Pharma公司生产,是仿制药。它只在南亚的印度、巴基斯坦和尼泊尔上市。目前尚未获准在中国大陆上市(未获...

格列卫能治疗这两种病
格列卫能治疗这两种病

格列卫是延长病人生命的神奇药物。实际上,格列卫主要用于治疗费城染色体阳性慢性髓细胞白血病(Ph+CML)的慢性期、加速期或急...

浅谈格列卫
浅谈格列卫

格列卫的主要功效:...

购买印度格列卫的渠道
购买印度格列卫的渠道

癌症是对人类健康的最大威胁,世界上每一分钟,都有许多病人为癌症所困扰。格列卫是治疗癌症的常用靶向药物,它能抑制肿瘤的...

格列卫的副作用
格列卫的副作用

白血病是一种血液病,也称为血癌,治疗非常困难。骨髓移植是一种方法,但患者往往选择其他治疗方法,因为他们找不到合适的骨...

印度格列卫很有效
印度格列卫很有效

格列卫是世界上首款真正意义上的癌症靶向药,是瑞士诺华公司研发生产的,其主要成分是甲磺酸伊马替尼,用于治疗慢性粒细胞白...

格列卫视频
直肠癌能治愈吗?能活多久?
直肠癌能治愈吗?能活多久?

临床上直肠癌只要能够做到早期发现、早期治疗...

结直肠癌早期如何筛查
结直肠癌早期如何筛查

结直肠癌的早期筛查是预防结直肠癌的一种重要手段,但是要具体情况具体分析。...

直肠癌能治愈吗?
直肠癌能治愈吗?

乳腺癌并不等于死亡,可以带瘤生存,所以不要多多紧张、焦虑、绝望甚至盲目投医,应静下来考虑对策,做好治疗前的心理准备...

药房目录大全

Pharmacy Catalogue