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依维莫司

印度依维莫司

【 药品别名 】 依维莫司 Everolimus

【药品简介】 依维莫司是一种mTOR的抑制剂,PI3K/AKT通路下游的一种丝氨酸苏氨酸激酶。在几种人癌症中mTOR失调控,依维莫司结合至细胞内蛋白,FKBP-12,导致一种抑制剂性复合物形成和mTOR激酶活性的抑制。依维莫司减低S6核糖体蛋白激酶(S6K1)的活性和真核生物延伸因子4E-结合蛋白(4E-BP),mTOR的下游效应器,涉及蛋白质合成。此外,依维莫司抑制缺氧-可诱导因子的表达(如,HIF-1)和减低血管内皮生长因子(VEGF)的表达。

【适应症状】 1) 雌激素受体阳性,her2阴性乳腺癌 依维莫司联合依西美坦,用于雌激素受体阳性,HER2阴性的绝经后妇女,并且用来曲唑或阿那曲唑治疗失败后的乳腺癌患者。 2) 神经内分泌瘤 依维莫司适用于成人患者,治疗进展,分化良好,非功能性的胃肠道(GI)或肺部起源的,不可切除、局部进展或转移性神经内分泌瘤,。 3) 舒尼替尼、索拉非尼治疗失败后的肾细胞癌 4)结节性硬化症(TSC)相关肾血管平滑肌脂肪瘤 依维莫司适用于成人患者,治疗不需要立即手术的肾血管平滑肌脂肪瘤和TSC。 5) 结节性硬化症复合物(TSC)相关的肾血管肌脂肪瘤 依维莫司适用于成人和1岁以上儿童,治疗需要治疗性干预但不能根治性切除的结节性硬化症(TSC)相关的室管膜巨细胞星形细胞瘤(SEGA)。 6)结节性硬化症复合物(TSC)相关发作性癫痫 依维莫司适用于成人和2岁及以上的儿童,作为结节性硬化症复合物(TSC)相关的部分发作性癫痫的辅助治疗。

印度依维莫司(依维莫司 Everolimus)价格,正品图片,治疗胰腺癌药物, 购买依维莫司请到印度药房官方网站进行购买 【印度药房大全目录】

资料发布时间:2018-10-30 14:50:00 资料更新时间:2019-11-12 09:05:54

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【印度依维莫司(依维莫司 Everolimus)说明书】

【依维莫司药品特色】   

在体外和或体内研究中通过依维莫司mTOR的抑制作用显示减低细胞增殖,抑制血管生成和葡萄糖摄取。依维莫司适用于用舒尼替尼或索拉非尼治疗失败后晚期肾细胞癌患者的治疗。

【用法用量】

推荐剂量:

1)  激素受体阳性,HER2阴性乳腺癌

依维莫司的推荐剂量为10mg,口服,每日一次,直至疾病进展或出现不可耐受的毒性。
 

2)  神经内分泌肿瘤(NET)

依维莫司的推荐剂量为10mg,口服,每日一次,直至疾病进展或出现不可耐受的毒性。
 

3)肾细胞癌(RCC)

依维莫司的推荐剂量为10mg,口服,每日一次,直至疾病进展或出现不可耐受的毒性。
 

4)结节性硬化症复合物(TSC)相关的肾血管肌脂肪瘤

依维莫司的推荐剂量为10mg,口服,每日一次,直至疾病进展或出现不可耐受的毒性。
 

5)结节性硬化症复合物(TSC)相关的室管膜细胞星形细胞瘤(SEGA)

依维莫司的推荐剂量为4.5 mg/m2 ,口服,每日一次,直至疾病进展或出现不可耐受的毒性。
 
依维莫司

6)结节性硬化症复合物(TSC)相关发作性癫痫

依维莫司的推荐剂量为5 mg/m2 ,口服,每日一次,直至疾病进展或出现不可耐受的毒性。
 
【不良反应】

1)感染性肺炎。

2)口腔炎。

3)  代谢异常:高血糖或血脂异常。

4)血小板减少;中性粒细胞减少;发热性中性粒细胞减少。

5)其他非血液性毒性。
 
依维莫司英文说明

Everolimus uses

Everolimus is used in breast cancer, pancreatic cancer, lung cancer and kidney cancer.

How everolimus works

Everolimus suppresses the activity of body's immune system and prevents rejection of the transplanted organ.

Common side effects of everolimus

Weakness, Sinus inflammation, Infection, Fever, Cough, Fatigue, Stomatitis (Inflammation of the mouth), Otitis media (infection of ear), Diarrhea, Upper respiratory tract infection

Everolimus

生物活性

产品描述

Everolimus is a potent mTOR inhibitor that binds to FKBP-12. It is used alone or in combination with calcineurin inhibitors.

靶点活性

mTOR (FKBP12),1.6nM-2.4nM

实验溶液

30% propylene glycol, 5% Tween 80, 65% D5W: 5 mg/mL

体外活性

Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 (IC50: 0.12-1.8 nM) [1]. RAD001 inhibited proliferation in vitro (IC50 values<1 nM to >1 μM), and pS6 kinase and 4E-BP1 were inhibited. In vitro, RAD001 inhibited the proliferation of VEGF-stimulated and fibroblast growth factor-stimulated human endothelial cells [2]. Everolimus exhibited a dose-dependent inhibition in both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells. The IC50 values of everolimus for BT474 and the primary CSCs were 2,054 and 3,227 nM, or 29 times and 21 times greater than the IC50 values for their corresponding total cells, respectively [3].

体内活性

In vivo, in tumor models derived from either sensitive or insensitive cells, RAD001 reduced Tie-2 levels, the amount of mature and immature vessels, total plasma, and tumor VEGF. RAD001 did not affect blood vessel leakiness in normal vasculature acutely exposed to VEGF nor did it affect tumor vascular permeability[2]. Compared to the control group, the everolimus, trastuzumab, and drug combination groups showed significant reductions in mean tumor sizes. Compared to the mean xenograft tumor size in the trastuzumab group, the mean tumor size in the everolimus group was larger. When the two drugs were combined, the xenograft tumor size was smaller than those of the groups treated with everolimus or trastuzumab alone [3].

激酶实验

FKBP12 binding assay & Mixed lymphocyte reaction (MLR) : FKBP12 binding assay: Binding to the FK 506 binding protein (FKBP12) is indirectly assessed by means of an ELISA-type competition assay. FK 506 is included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to FK 506 (rIC50 = IC50 Everolimus/IC50 FK 506). Mixed lymphocyte reaction (MLR): The immunosuppressive activities of RAP and its derivatives are assessed in a two-way MLR, using spleen cells of BALB/c and CBA mice. RAP is included in each individual experiment as a standard, and the inhibitory activity is expressed as relative IC50 compared to RAP (rIC50 = IC50 Everolimus/IC50 RAP).

细胞实验

The 3-(4-5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide dye reduction assay (MTT assay) is used to compare the effects of Everolimus or trastuzumab on total breast cancer cells and breast CSCs. The total cells and the stem cells from the BT474 cell line and the primary breast cancer cells are respectively seeded into 96-well plates with different concentrations of the drugs, with five wells for each concentration, and the cells are cultured at 37 °C with 5 % CO2 in an incubator for 24 hours. The concentrations of Everolimus are 1 nM, 10 nM, 100 nM, 1 μM and 10 μM, and the concentrations of trastuzumab are 0.5 μg/mL, 1 μg/mL, 10 μg/mL, 50 μg/mL, and 100 μg/mL. The combinatorial inhibitory effect of Everolimus and Trastuzumab on the in vitro growth of breast CSCs is examined by MTT assay as well using 10 μg/mL trastuzumab in combination of increasing concentrations of everolimus (1 nM, 10 nM, 100 nM and 1 μM). After drug treatment for 24 hours, 20 μL MTT [5 mg/mL in phosphate buffered saline (PBS)] is added to each well, and the cells are incubated at 37 °C with 5 % CO2 and saturated humidity for 4 hours. Following the subsequent removal of the supernatant, 150 μL dimethyl sulfoxide (DMSO) is added to each well, and the cells are vortexed for 10 minutes. The light absorbance (OD value) is measured for each well using an ELISA reader. Each experiment is repeated in triplicate, and dose–response curves are plotted. The probit software of the statistical software package SPSS 17.0 for Windows is used to calculate the inhibitory concentration (IC50) of Everolimus.(Only for Reference)

细胞系: BT474 cell line and the primary breast cancer cells

动物实验

动物模型:Cultured BT474 stem cells are injected beneath the left breast pad of BALB/c nude mice.

化学信息

分子量

958.22

分子式

C53H83NO14

CAS

159351-69-6

溶解度

Ethanol: 7 mg/mL (7.3 mM)

DMSO: 30 mg/mL (31.3 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 1.044 ml 5.218 ml 10.436 ml
5 mM 0.209 ml 1.044 ml 2.087 ml
10 mM 0.104 ml 0.522 ml 1.044 ml
50 mM 0.021 ml 0.104 ml 0.209 ml
参考文献
 
1. Sedrani R, et al. Chemical modification of rapamycin: the discovery of SDZ RAD. Transplant Proc. 1998 Aug;30(5):2192-4.
2. Lane HA, et al. mTOR inhibitor RAD001 (everolimus) has antiangiogenic/vascular properties distinct from a VEGFR tyrosine kinase inhibitor. Clin Cancer Res. 2009 Mar 1;15(5):1612-22.
3. Zhu Y, et al. Antitumor effect of the mTOR inhibitor everolimus in combination with trastuzumab on human breast cancer stem cells in vitro and in vivo. Tumour Biol. 2012 Oct;33(5):1349-62.
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