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阿昔替尼

印度阿昔替尼

资料发布时间:2018-10-30 14:50:00 最后更新时间:2020-03-27 09:59:21

【药品简介】 阿昔替尼能抑制酪氨酸激酶受体包括血管内皮生长因子受体(VEGFR)-1,VEGFR-2和VEGFR-3。阿西替尼通过同这些受体结合,从而抑制肿瘤血管生成,减缓肿瘤生长和病情进展。

【适应症状】 阿昔替尼,本品为抗肿瘤药,临床上主要用于既往接受过一种酪氨酸激酶抑制剂或细胞因子治疗失败的进展期肾细胞癌(RCC)的成人患者。

【 药品别名 】 阿昔替尼 Axitinib Inlyta

印度阿昔替尼(阿昔替尼 Axitinib Inlyta)价格,正品图片,治疗肾癌药物, 购买阿昔替尼请到印度药房官方网站进行购买 【印度药房大全目录】

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【印度阿昔替尼说明书,怎么吃?】

【用法用量】
 
1)阿昔替尼开始剂量为5mg,口服,每天2次。可根据个体安全性和耐受性调整阿昔替尼剂量。
 
2)约间隔12小时给予阿昔替尼剂量有或无食物。
 
3)阿昔替尼应予一杯水整片吞服。
 
4)如需要强CYP3A4/5抑制剂,减低阿昔替尼剂量约半量。
 
5)对中度肝受损患者,减低开始阿昔替尼剂量约半量。
 

【不良反应】
 
阿昔替尼最常见(≥20%)不良反应是腹泻,高血压,疲乏,食欲减低,恶心,发音障碍,手掌-足底综合征,体重减轻,呕吐,乏力,和便秘。
 
阿昔替尼
 
 
【注意事项】
 
1)阿昔替尼曾观察到高血压包括高血压危象。开始阿昔替尼前应充分控制血压。需要监视和治疗高血压。尽管使用抗高血压药物,对持续高血压减低阿昔替尼剂量。
 
2)阿昔替尼曾观察到动脉和静脉血栓事件和阿昔替尼可能致死。对这些事件风险增加患者慎用阿昔替尼。
 
3)阿昔替尼曾报道出血事件,包括致命性事件。阿昔替尼尚未在未治疗脑转移或最近活动性胃肠道出血证据患者中研究过阿昔替尼和在这些患者中不应使用阿昔替尼。
 
4)阿昔替尼曾发生胃肠道穿孔和瘘管,包括死亡。对胃肠道穿孔或瘘管风险患者慎用阿昔替尼。
 
5)阿昔替尼曾报道甲状腺低下症需要甲状腺激素替代。用阿昔替尼治疗开始前监视甲状腺功能,和自始至终定期。
 
6)计划手术前至少24小时停止阿昔替尼。
 
7)曾观察到可逆性后部白质脑病综合征(RPLS),如发生RPLS体征或症状永久终止阿昔替尼。
 
8)用阿昔替尼治疗开始前,和自始至终定期监视蛋白尿。对中度至严重蛋白尿,减低阿昔替尼剂量或暂时中断用阿昔替尼治疗。
 
9)用阿昔替尼治疗时曾观察到肝酶升高。用阿昔替尼治疗开始前和自始至终定期监视ALT,AST和胆红素。
 
10)中度肝受损患者如使用阿昔替尼开始剂量应减低阿昔替尼。严重肝受损患者中未曾研究过阿昔替尼。
 
11)当给予妊娠妇女根据其作用机制阿昔替尼可能致胎儿危害。应忠告生育能力妇女阿昔替尼对胎儿潜在危害和当接受阿昔替尼避免成为妊娠。


Axitinib uses

Axitinib is used in the treatment of kidney cancer.

How axitinib works

Axitinib 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 axitinib

Headache, Nausea, Rash, Breathing difficulty, Joint pain, Difficulty in speaking, Decreased level of thyroid hormones, Pain in extremity, Haemorrhage, Vomiting, Abdominal pain, Dyspepsia, Dry skin, Diarrhea, High blood pressure, Decreased appetite, Cough, Taste change, Painful blisters on hands and feet, Constipation, Stomatitis (Inflammation of the mouth), Protein in urine

Axitinib

生物活性

产品描述

Axitinib is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively.

靶点活性

PDGFRβ,1.6 nM

VEGFR1/FLT1,0.1 nM

VEGFR2/Flk1,0.18 nM

VEGFR2/KDR,0.2 nM

VEGFR3,0.1-0.3 nM

Kit,1.7 nM

实验溶液

0.5% CMC: 30 mg/mL

体外活性

In transfected or endogenous RTK-expressing cells, axitinib potently blocked growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 (IC50s: 0.2 and 0.1 to 0.3 nmol/L, respectively). Cellular activity against VEGFR-1 was 1.2 nmol/L. Axitinib rapidly and dose-dependently reduced the phosphorylation of Akt, endothelial nitric oxide synthase (eNOS), and extracellular signal-regulated kinase 1/2 (ERK1/2), key downstream signaling molecules of VEGF [1]. Axitinib reduced cell viability in a dose-dependent manner with IC50 doses of >10,000, 849 and 274 nmol/l for IGR-N91, IGR-NB8, and SH-SY5Y, respectively. the sensitivity to axitinib of neuroblastoma cell lines appeared to be in a similar range as non-VEGF stimulated HUVEC (IC50: 573 nmol/l) [2].

体内活性

Acute axitinib treatment rapidly and significantly reduced retinal vascular VEGFR-2 phosphorylation. One hour after the second dose, retinal VEGFR-2 phosphorylation was reduced by 80% to 90% compared with that of the control tissues. Six and 24 to 32 h post-dose, the phospho-VEGFR-2 levels returned to 50% and 100% of the control, respectively. The EC50 value for the inhibition of VEGFR-2 phosphorylation was 0.49 nmol/L [1]. Mice were next treated for a period of 2 weeks with either fractionated radiation (5 × 2 Gy/wk) or AG-013736 (25 mg/kg/d) and 1 to 3 weeks for the combination. Tumor volume at the end of 2 weeks was significantly reduced for either single or combination treatments. Percentage increases in tumor volume were similar between radiotherapy (40 ± 9.8%) and AG-013736 (48 ± 9.2%), and the combination was markedly reduced versus controls (12 ± 5.7% versus 77 ± 11%) [3].

激酶实验

Porcine aorta endothelial (PAE) cells overexpressing full-length VEGFR-2, PDGFR-β, KIT, and NIH-3T3 overexpressing murine VEGFR-2 (Flk-1) or PDGFR-α were generated as described previously. The ELISA capture plates were prepared by coating 96-well ReactiBind plates with 100 μL/well of 2.5 μg/mL anti-VEGFR-2 antibody, 0.75 μg/mL anti-PDGFR-β antibody, 0.25 μg/mL anti-PDGFR-α antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody. Measurement of RTK phosphorylation by ELISA was done as described previously [1].

细胞实验

Endothelial or tumor cells were starved for 18 h in the presence of either 1% FBS (HUVEC) or 0.1% FBS (tumor cells). Axitinib was added and cells were incubated for 45 min at 37°C in the presence of 1 mmol/L Na3VO4. The appropriate growth factor was added to the cells, and after 5 min, cells were rinsed with cold PBS and lysed in the lysis buffer and a protease inhibitor cocktail. The lysates were incubated with immunoprecipitation antibodies for the intended proteins overnight at 4°C. Antibody complexes were conjugated to protein A beads and supernatants were separated by SDS-PAGE. The Super Signal West Dura kit was used to detect the chemiluminescent signal [1].

细胞系: HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells

动物实验

AG-013736, a receptor kinase inhibitor of VEGFRs and, at higher doses, PDGFRs (IC50 = 0.1 nmol/L for VEGFR-1, 0.2 nmol/L for VEGFR-2, 0.1–0.3 nmol/L for VEGFR-3, and 1.6 nmol/L for PDGFRβ; ref. 18), was provided by Pfizer Global Research and given once daily by gavage in a volume of 0.13 mL. Control animals received 0.5% carboxymethylcellulose drug carrier. Irradiations were done on nonanesthetized mice using a 137Cs source operating at 2.4 Gy/min. Mice were confined to plastic jigs with tumor-bearing legs extended through an opening in the side, allowing local irradiations. Fractionated doses were given in five daily 2 Gy fractions per week (omitting weekends). For combination treatments, radiotherapy was delivered first, and AG-013736 was given within ?4 h. Mice were sacrificed, and tumors were excised and then quick frozen (using liquid nitrogen) following 1, 2, or 3 weeks of treatment [3].

动物模型:BT474 breast cancer cells are implanted subcutaneously into Immune-deficient femice (Nu/nu; age 8-12 weeks).

化学信息

分子量

386.47

分子式

C22H18N4OS

CAS

319460-85-0

溶解度

DMSO: 9.7 mg/mL (25 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 2.588 ml 12.938 ml 25.875 ml
5 mM 0.518 ml 2.588 ml 5.175 ml
10 mM 0.259 ml 1.294 ml 2.588 ml
50 mM 0.052 ml 0.259 ml 0.518 ml

参考文献
 
1. Hu-Lowe DD, et al. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Clin Cancer Res. 2008 Nov 15;14(22):7272-83.
2. R?ssler J, et al. The selective VEGFR1-3 inhibitor axitinib (AG-013736) shows antitumor activity in human neuroblastoma xenografts. Int J Cancer. 2011 Jun 1;128(11):2748-58.
3. Fenton BM, et al. The addition of AG-013736 to rractionated radiation improves tumor response without functionally normalizing the tumor vasculature. Cancer Res. 2007 Oct 15;67(20):9921-8.

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