您的位置: 印度药房网 > 医药大数据 > 结直肠癌 >
瑞格非尼

印度瑞格非尼

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-08-13 10:10:24

【药品简介】 瑞戈菲尼可广泛抑制与血管生成和肿瘤发生相关的激酶

【适应症状】 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、伊立替康方案的化疗或抗VEGF药物或抗EGFR药物(如果患者是RAS野生型)的转移性结直肠癌。胃肠道间质性肿瘤:用于治疗既往曾用伊马替尼和舒尼替尼药物的,局部进展的、无法切除的或转移性胃肠道间质性肿瘤(GIST)

【 药品别名 】 拜万戈 瑞戈非尼 Stivarga regorafenib

印度瑞格非尼(拜万戈 瑞戈非尼 Stivarga regorafenib)价格,正品图片,治疗结直肠癌药物, 购买瑞格非尼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

【印度瑞格非尼说明书,怎么吃?】

【作用机制】   

拜万戈瑞戈非尼)是一个多激酶抑制剂,通过抑制肿瘤血管生成、肿瘤细胞新生、维持肿瘤微环境的因素,来抑制肿瘤生长。包括VEGF受体1-3,KIT,PDGFR-alpha,PDGFR-beta,RET,FGFR1和2,TIE2,DDR2,TrkA,Eph2A,RAF-1,BRAF,BRAF-V600E,SAPK2,PTK5和Abl。
 
【副作用】 

乏力,食欲减轻,皮肤反应,腹泻,口腔黏膜炎,体重减轻,感染,高血压,发音困难等。

【给药方法】

口服,每天定时服药。低脂饮食后,用水吞服。

【参考用法】

口服,160mg,每天一次,28天为一个周期,在前21天服用(服用21天,休息7天),直至疾病进展或不可接受的毒性。

【注意事项】

使用瑞格菲尼后,因副反应可调整剂量:在原有基础上可每次减少一片药:40mg。每日最少推荐剂量为80mg。
瑞格非尼

【在以下情况时应当永久停止使用瑞格菲尼】

使用80mg的剂量时,仍不能耐受。

任何情况下发生ALT或AST升高至正常值上限的20倍以上时。

任何情况下发生ALT或AST升高至正常值上限的3倍以上,且伴有胆红素高于正常值上限值的2倍。

即使将剂量减少至120mg,再次发生ALT或AST升高至正常值上限的5倍以上。

对于任何4级副反应,只有当潜在的益处大于风险时才能继续使用该药。

Regorafenib uses

Regorafenib is used in the treatment of cancer of colon and rectum.

How regorafenib works

Regorafenib is an anti-cancer medication. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps to stop or slow the spread of cancer cells.

Common side effects of regorafenib

Rash, Weakness, Low blood platelets, Difficulty in speaking, Haemorrhage, Vomiting, Pain, Nausea, Infection, Hair loss, Fever, Anemia (low number of red blood cells), Diarrhea, High blood pressure, Decreased appetite, Mucosal inflammation, Stomatitis (Inflammation of the mouth)

Regorafenib

生物活性

产品描述

Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).

靶点活性

Kit,7 nM (cell free)

Raf-1,2.5 nM (cell free)

RET,1.5 nM (cell free)

VEGFR1,13 nM (cell free)

VEGFR2,4.2 nM (cell free)

B-Raf (V600E),19 nM (cell free)

实验溶液

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

体外活性

Regorafenib potently inhibited a distinct set of kinases, including the angiogenic and stromal RTKs VEGFR1-3, TIE2, FGFR1 and PDGFR-b (IC50s: 4-311 nM), and the oncogenic RTKs KIT and RET, along with the intracellular signaling kinases c-RAF/RAF-1 and BRAF and its V600E mutant (IC50s: 1.5-28 nM). Regorafenib potently inhibited VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells (IC50: 3 nM). In HAoSMCs, regorafenib inhibited PDGFR-b autophosphorylation after stimulation with PDGF-BB (IC50: 90 nM) [1]. Regorafenib caused a concentration-dependent decrease in Hep3B cell growth (IC50: 5 μM). PLC/PRF/5 cells were similar in their responses to Hep3B cells, but HepG2 cells were more sensitive (IC50: 1 μM) [2].

体内活性

Treating tumor-bearing rats with a single oral dose of regorafenib at 10 mg/kg caused a significant decrease in tumor perfusion and extravasation of the contrast agent. A significant reduction of the normalized IAUC360 was observed by 10 hr after regorafenib treatment and persisted for up to 2 days when compared with vehicle. Regorafenib dosed qd orally inhibited tumor growth in a dose-dependent manner in multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors. Regorafenib (10–100 mg/kg) effectively inhibited the growth of the Colo-205 xenografts, reaching a TGI of ~75% at day 14 at the 10 mg/kg dose [1]. In murine xenograft models, oral regorafenib, M-2, and M-5 significantly inhibited tumor growth versus controls. Total peak plasma drug concentrations and exposure to M-2 and M-5 in mice after repeated oral dosing with regorafenib 10 mg/kg/day were comparable to those in humans [3].

激酶实验

In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFR-b (aa561–aa1106), RAF-1 (aa305–aa648) and BRAFV600E (aa409–aa765) kinase domains were performed as previously described. Initial in vitro kinase inhibition profiling was performed at a fixed 1 μM compound concentration under Millipore standard conditions [10 μM adenosine-50’- triphosphate (ATP) concentration]. Inhibitory concentration of 50% (IC50) values were determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition was measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.

细胞实验

Each cell line was seeded at 0.3×10^5 cells/2ml of DMEM containing 10% FBS in 35 mm tissue culture dishes. The cells were incubated for 24 h to allow attachment, and then the medium was replaced by fresh culture medium containing Regorafenib at increasing concentrations (1 μM, 2.5 μM, 5 μM, 7.5 μM and 10 μM). In these experimental conditions, the cells were allowed to grow for 72 or 96 h. Time-course experiments on Hep3B cells were performed with 7.5 μM of Regorafenib at short (15, 60, 180 min.), middle (24, 48, 72 and 96 h) or long times (up to seven days). When the cells were treated for long times the drug was replaced with a fresh one. Each experiment included a control with the equivalent concentration of DMSO (solvent control) as the one used for adding Regorafenib. Each experiment was performed in triplicate and repeated 3 times. Subsequent analyses were performed at specific Regorafenib concentrations and incubation times [2].

细胞系: GIST 882 and TT cells

动物实验

Female athymic NCr nu/nu mice, kept in accordance with Federal guidelines, were subcutaneously inoculated with 5×10^6 Colo-205 or MDAMB-231 cells or implanted with 1 mm^3 786-O tumor fragments. When tumors reached a volume of ~100 mm^3, regorafenib or vehicle control was administered orally qd×21 in the 786-O model, and qd×9 in the Colo-205 and MDA-MB231 models, respectively, at doses of 100, 30, 10, and 3 mg/kg. Paclitaxel was administered intravenously at 10 mg/kg in ethanol/Cremophor ELV/saline (12.5%/12.5%/75%) every 2 days×5. Tumor size (volume) was estimated twice weekly (l×w^2)/2, and the percentage of tumor growth inhibition (TGI) was obtained from terminal tumor weights (1-T/C100). Mice were weighed every other day starting from the first day of treatment. The general health status of the mice was monitored daily [1].

动物模型:Feathymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O

化学信息

分子量

482.82

分子式

C21H15ClF4N4O3

CAS

755037-03-7

溶解度

DMSO: 90 mg/mL (186.4 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 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 2.071 ml 10.356 ml 20.712 ml
5 mM 0.414 ml 2.071 ml 4.142 ml
10 mM 0.207 ml 1.036 ml 2.071 ml
50 mM 0.041 ml 0.207 ml 0.414 ml

参考文献
 
1. Wilhelm SM, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 2011, 129(1), 245-255.
2. Carr BI, et al. Fluoro-Sorafenib (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297.
3. Zopf D, et al. Pharmacologic activity and pharmacokinetics of metabolites of regorafenib in preclinical models. Cancer Med. 2016 Nov;5(11):3176-3185.
注:本站瑞格非尼(拜万戈 瑞戈非尼 Stivarga regorafenib)药品说明,价格,正品图片均来自于官方,瑞格非尼如何服用请尊医嘱。如需药品请到正规印度药房进行购买
上一篇:没有了 下一篇:格列卫
瑞格非尼相关药品
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...

瑞格非尼资讯
瑞戈非尼怎么服用
瑞戈非尼怎么服用

瑞戈非尼是第一个结束了索拉非尼唯一肝癌靶向药的新药物,能够 用作二线肝癌的治疗,由拜耳研发生产。 瑞戈非尼的原研药和拜...

瑞戈非尼能减少进展风险
瑞戈非尼能减少进展风险

各项医学研究早已经检验了瑞戈非尼的安全。CORRECT医学研究中瑞戈非尼组270例、安慰剂组35例出现3-4级医治有关不良反应,瑞戈非尼...

瑞戈非尼对于结直肠癌的疗效很好
瑞戈非尼对于结直肠癌的疗效很好

结直肠癌是世界上第三大最常见的癌症,每年新增136万例。5年生存期在28%65%之间。过去,转移性直肠癌的主要医治手段以化疗和手术...

瑞戈非尼的用法用量
瑞戈非尼的用法用量

瑞戈非尼现阶段主要是使用于胃肠间质瘤和转移性结肠癌的靶向药物治疗。较于安慰剂组,可让受到标准医治后肿瘤处于进展情况期...

服用瑞戈非尼需要注意这些
服用瑞戈非尼需要注意这些

瑞戈非尼实际上是一个较为新型的抗肿瘤药物,具体的成分便是瑞戈非尼,是一个淡粉色椭圆形薄膜衣片,为口服多激酶抑制剂。...

瑞戈非尼的副作用有这些
瑞戈非尼的副作用有这些

结直肠癌早期无明显表现,近年来患病率逐年上升,但可采取的治疗方法相对有限。瑞戈非尼是该国为数不多的可用于治疗该病的药...

瑞戈非尼的临床试验效果
瑞戈非尼的临床试验效果

肝癌具有较高的发病率和死亡率。由于该病早期缺乏具体症状,发病隐匿,早期易被忽视或误诊。许多患者在确诊时已发展为晚期肝...

乐伐替尼耐药后,用瑞戈非尼?
乐伐替尼耐药后,用瑞戈非尼?

乐伐替尼耐药后怎么办?二线用药卡博替尼...

瑞戈非尼的作用
瑞戈非尼的作用

瑞戈非尼是获批用于肝癌二线医治的药物,也是今朝二线医治药物...

瑞戈非尼怎么抑制肿瘤
瑞戈非尼怎么抑制肿瘤

甚么是瑞戈非尼?瑞戈非尼与索拉非尼(多吉美)都是一种口服多激酶物质...

瑞格非尼视频
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