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恩杂鲁胺

恩杂鲁胺

【 药品别名 】 恩杂鲁胺 Enzalutamide

【药品简介】 恩杂鲁胺(Enzalutamide)是一种雄激素受体抑制剂,它作用于雄激素受体信号通路的步骤不同。研究表明,苯丙胺能抑制雄激素受体与雄激素受体的结合,抑制雄激素受体的核易位和与DNA的相互作用。

【适应症状】 恩杂鲁胺适用于抗肿瘤药多西他赛治疗后的前列腺癌患者。

印度恩杂鲁胺(恩杂鲁胺 Enzalutamide)价格,正品图片,治疗前列腺癌药物, 购买恩杂鲁胺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 09:15:16

【印度恩杂鲁胺(恩杂鲁胺 Enzalutamide)说明书】

【用法用量】

推荐剂量:160 mg (4 片*40 mg胶囊)口服每日一次;可以带或不带食物吞下胶囊;不要咀嚼、溶解或打开胶囊

【不良反应】

恩杂鲁胺最常见不良反应(≥5%)是虚弱/疲劳,背痛,腹泻,关节痛,潮热,外周血水肿,肌肉骨骼痛,头痛,上呼吸道感染,肌肉无力,眩晕,失眠,下呼吸道感染,脊髓压迫症和马尾神经综合征,血尿,感觉异常,焦虑,和高血压。
 
【注意事项】

1.妊娠妇女禁用恩杂鲁胺。

2.接受恩杂鲁胺患者0.9%发生癫痫发作。没有曾有癫痫发作患者,在有癫痫发作诱发因素患者,或同时使用药物可能降低癫痫发作阈患者中使用恩杂鲁胺的恩杂鲁胺临床试验经验。
恩杂鲁胺

Enzalutamide uses

Enzalutamide is used in the treatment of prostate cancer.

How enzalutamide works

Enzalutamide is an antiandrogens. It works by blocking the effect of the natural male hormones on the growth of prostate cells.

Common side effects of enzalutamide

Headache, Hot flashes, Weakness, High blood pressure, Fatigue

Enzalutamide 

生物活性

产品描述

Enzalutamide (MDV 3100) is a non-steroidal androgen receptor (AR) antagonist (IC50: 36 nM in LNCaP prostate cells).

靶点活性

Androgen Receptor,36nM

实验溶液

2% DMSO+30% PEG300: 5 mg/mL

体外活性

Enzalutamide (MDV 3100) bound AR in castration-resistant LNCaP/AR human prostate cancer cells with 5-8 fold greater affinity than bicalutamide. MDV3100 antagonized induction of PSA and TMPRSS2 by the synthetic androgen R1881 in parental LNCaP cells. In the human prostate cancer cell line VCaP which has endogenous AR gene amplification, MDV3100 suppressed growth and induced apoptosis [1].

体内活性

Enzalutamide (10 mg/kg) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts [1]. After intravenous injection (Enzalutamide, 0.5-5 mg/kg), systemic clearance, volumes of distribution at steady state (Vss), and half-life (T½) remained unaltered as a function of dose, with values in the ranges of 80.4-86.3 mL/h/kg, 1020-1250 mL/kg, and 9.13-10.6 h, respectively. Following oral administration, absolute oral bioavailability was 89.7 % and not dose-dependent [2].

激酶实验

AR reporter assay: Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of Enzalutamide is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to Enzalutamide treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of Enzalutamide. After two days of incubation, reporter activities are assayed.

细胞实验

For in vitro experiments, LNCaP or LNCaP/AR cells (10^4 cells/well) were androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells were challenged with various concentrations of R1881, bicalutamide, RD162 or MDV3100 in media containing 5-10% charcoal-stripped serum [1].

细胞系: LNCaP or LNCaP/AR cells

动物实验

In vivo tumorigenicity experiments were done by subcutaneous injection of 10^6 cells (100 uL in 50% Matrigel and 50% growth media) into the flanks of castrated male SCID mice. Daily gavage treatment (using a formulation of 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO) was initiated when tumor size reached ~100 mm3. Tumor size was measured weekly in three dimensions (l x w x d) with calipers. For in vivo luciferase imaging, d-luciferin substrate (100 μL, 15 mg/mL) was injected intraperitoneally. After 5 minutes, mice were anesthetized using isofluorane and imaged using a cooled charged-coupled device IVIS camera. Data were analyzed using Living Image 2.30 software [1].

动物模型:Castration-resistant LNCaP/HR xenografts in SCID mice

化学信息

分子量

464.44

分子式

C21H16F4N4O2S

CAS

915087-33-1

溶解度

DMSO: 85 mg/mL (183 mM)

Ethanol: <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 2.153 ml 10.766 ml 21.531 ml
5 mM 0.431 ml 2.153 ml 4.306 ml
10 mM 0.215 ml 1.077 ml 2.153 ml
50 mM 0.043 ml 0.215 ml 0.431 ml

参考文献
 
1. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790.
2. Kim TH, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82.
注:本站恩杂鲁胺(恩杂鲁胺 Enzalutamide)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
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