您的位置: 印度药房网 > 医药大数据 > 乳腺癌 >
Everolimus

Everolimus

【 药品别名 】 依维莫司 Everolimus

【药品简介】 Everolimus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,Everolimus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。Everolimus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Everolimus(依维莫司 Everolimus)价格,正品图片,治疗乳腺癌药物, 购买Everolimus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 09:16:53

【印度Everolimus(依维莫司 Everolimus)说明书】

【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。Everolimus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:
Everolimus
 
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。
 
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。

Everolimus
 
【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。
 

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.
注:本站Everolimus(依维莫司 Everolimus)药品说明均来自于官方,请咨询您的治疗医生了解更多细节。如需药品请到正规印度药房进行购买
上一篇:赫赛汀 下一篇:拉帕替尼
Everolimus相关药品
帕博西尼
帕博西尼

帕博西尼与来曲唑治疗绝经后妇女的雌激素受体(ER)阳性,人表皮生长因子受体2(HER2)阴性晚期乳腺癌,作为初始内分泌为基础的治疗...

Olaparib
Olaparib

1)复发卵巢癌的维持治疗: ①对于上皮性复发性卵巢癌成人患者的维持治疗 ②对铂类敏感或部分敏感的输卵管或原发性腹膜癌的化...

赫赛汀
赫赛汀

Hertraz适用于治疗HER2过表达的转移性乳腺癌和转移性胃癌。 1、Hertraz作为单一药物治疗已接受过1个或多个化疗方案的转移性乳腺癌。...

Everolimus
Everolimus

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...

拉帕替尼
拉帕替尼

乳腺癌:拉帕替尼用于联合卡培他滨治疗ErbB-2过度表达的,既往接受过包括蒽环类,紫杉醇,曲妥珠单抗(赫赛汀)治疗的晚期或转移性乳...

Everolimus资讯
使用拉帕替尼治疗乳腺癌需要注意这些
使用拉帕替尼治疗乳腺癌需要注意这些

拉帕替尼用于治疗晚期激素相关乳腺癌,与其他癌症药物治疗后进展或扩散。只有当肿瘤检测为人表皮生长因子受体2(HER2)蛋白阳...

依维莫司多少钱?适应症及疗效
依维莫司多少钱?适应症及疗效

依维莫司是当前唯一一款mTOR抑制剂并被广泛运用到多种实体肿瘤的治疗上,原产自瑞士诺华,2013年在国内上市,但价格比较昂贵,...

服用依维莫司要知道这些
服用依维莫司要知道这些

依维莫司主要用于治疗接受过舒尼替尼或者索拉菲尼治疗失败的晚期肾癌细胞患者,和不可切除局部晚期的或者转移性、分化良好的...

依维莫司的副作用
依维莫司的副作用

依维莫司是一种选择性激酶抑制剂。2009年在美国首次获得批准用于晚期肿瘤的治疗,2013年在中国上市,2014年批准用于晚期胰腺神经...

依维莫司的用药须知
依维莫司的用药须知

依维莫司2009年被FDA批准治疗肾癌,2012年批准与依西美坦联合治疗激素受体阳性,HER2基因阴性晚期乳腺癌患者。依维莫司有着很好的...

Palbociclib,乳腺癌的治疗
Palbociclib,乳腺癌的治疗

帕博西尼适应症用于治疗乳腺癌,其他适应症正在进行临床试验(非小细胞肺癌、淋巴瘤、多发性骨髓瘤)。帕博西尼胶囊:帕博西尼...

乳腺癌靶向药
乳腺癌靶向药

乳腺癌是全世界女性癌症死亡的主要原因。对于乳腺癌的治疗,靶向药物越来越受到重视。无数乳腺癌患者期待更好的治疗。...

印度依维莫司的用法和适应症
印度依维莫司的用法和适应症

癌症一直都是威胁着人类生命的重大疾病,现在随着医学的不断发展,出现了一些针对多种癌症的靶向药,今天给大家介绍的这款依...

依维莫司效果很好
依维莫司效果很好

依维莫司的原药厂是瑞士诺华,依维莫司的主要用途之一是肾癌,依维莫司能治疗的适应症比较多,疗效明显。依维莫司在2009年3月...

依维莫司的抗癌范围很广
依维莫司的抗癌范围很广

依维莫司是瑞士诺华公司研发的靶向药物。商品名称:飞尼妥。依维莫司是mTOR的选择性抑制剂。小编了解到,除了原版的依维莫司外...

Everolimus视频
什么是白血病?
什么是白血病?

白血病是一类造血干细胞恶性克隆性疾病...

中医与免疫治疗有什么关系?
中医与免疫治疗有什么关系?

中医有一句话叫做正气存内邪不可干,正气就包括了阴阳的平衡,气血、脏腑功能的平衡...

宝宝得了白血病还有救吗?
宝宝得了白血病还有救吗?

宝宝得了白血病不光有救,也有可能完全治愈,...

儿童白血病如何治疗?
儿童白血病如何治疗?

儿童白血病的治疗原则为早期诊断、早期治疗,有间歇、交替用药的方式,并坚持长期的治疗,预防复发。...

药房目录大全

Pharmacy Catalogue