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奥拉帕尼

印度奥拉帕尼

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

【药品简介】 奥拉帕尼是多聚二磷酸腺苷核糖聚合酶(PARP)抑制剂,用于治疗BRCA基因突变的肿瘤, 比如卵巢癌,乳腺癌,前列腺癌。PARP酶涉及细胞的正常功能,如DNA的转录和 DNA修复。美国药监局临床研究显示:奥拉帕尼无论是作为单药治疗或联合铂类为基础的化疗,均能够抑制试管中肿瘤细胞的生长,和减少人类肿瘤的生长

【适应症状】 奥拉帕尼,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疗。 2)接受3线或以上化疗方案后仍有进展的gBRCA基因突变的晚期卵巢癌。 3)BRCA基因突变的HER2阴性的转移性乳腺癌:①曾接受新辅助化疗、辅助化疗、转移性化疗的有害或可疑有害的gBRCA基因突变、HER2阴性的转移性乳腺癌患者②激素受体阳性的患者需先进行内分泌治疗,不适合用内分泌治疗的患者再用奥拉帕尼。

【 药品别名 】 奥拉帕尼 Olaparib

印度奥拉帕尼(奥拉帕尼 Olaparib)价格,正品图片,治疗卵巢癌药物, 购买奥拉帕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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【印度奥拉帕尼说明书,怎么吃?】

【用法用量】
 
推荐剂量:300mg,口服,每日两次,每天的总剂量为600mg。
 
服用方法:口服,饭前饭后均可。整片吞咽,不要咀嚼、压碎、溶解或分割药片
 
治疗时间:继续治疗直到疾病进展或不可接受的毒性。
 

【不良反应】
 
最常见的奥拉帕尼不良反应(≥20%)是贫血,恶心,乏力,呕吐,腹泻,味觉障碍,消化不良,头痛,食欲下降,鼻咽炎/咽炎/URI,咳嗽,关节痛或肌肉骨骼痛,肌痛,背部疼痛,皮炎或皮疹和腹痛或不适。
 
最常见的奥拉帕尼实验室检查异常(≥25%)为提高肌酐,平均红细胞体积升高,降低血红蛋白,降低淋巴细胞,减少中性粒细胞绝对计数,并减少血小板。
 
 
 
【注意事项】
 
1)骨髓增生异常综合征或急性髓系白血病(MDS/AML)患者发生接触奥拉帕尼有些情况下是致命的,监测患者的血液学毒性。
 
2)肺炎:如果肺炎确认停止奥拉帕尼。
 
3)胚胎胎儿毒性:奥拉帕尼可引起胎儿危害。奉劝女性奥拉帕尼的潜在风险繁殖潜力的一个胎儿,避免怀孕。
 

Olaparib uses

Olaparib is used in the treatment of ovarian cancer.

How olaparib works

Olaparib is an anticancer medication. It works by stopping Poly-ADP-ribose polymerase (PARP) from working. PARP is a protein that helps cancer cells to repair themselves and continue to survive.

Common side effects of olaparib

Nausea, Vomiting, Decreased blood cells (red cells, white cells, and platelets), Abdominal pain, Dizziness, Weakness, Sore throat, Runny nose, Diarrhea, Joint pain, Muscle pain, Back pain, Headache, Constipation, Mouth sore, Respiratory tract infection, Taste change,

Loss of appetite, Indigestion, Heartburn

Olaparib

生物活性

产品描述

Olaparib is a small molecule inhibitor of PARP1/PARP2 (IC50: 5/1 nM) but is less effective against the PARP tankyrase-1 (IC50: 1.5 μM).

靶点活性

PARP1,5 nM (cell free)

PARP2,1 nM (cell free)

实验溶液

15% Captisol: 15 mg/mL

体外活性

Following the establishment of a growth-inhibition curve for MMS on SW620 cells, the addition of the PARP-1 inhibitor at nM concentrations dose-dependently increased the effectiveness of MMS. Olaparib (AZD2281) was applied to SW620 cell lysates at a similar concentration range and identified the IC50 for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30-100 nM [1]. Concentrations of cisplatin capable of suppressing cell survival by 90% in the presence of 0, 1 or 3 μM AZD2281 were approximately 2.1, 1.5, and 1.2 μM in HSC-2 cells, 1.7, 1.4, and 0.98 μM in Ca9-22 cells, and 2.4, 1.5 and 1.3 μM in SAS cells, respectively. The combination of 1 μM cisplatin and 1 μM AZD2281 attenuated growth rates compared with single treatments of either cisplatin or AZD2281 [2]. The largest difference in drug sensitivity between BRCA2-deficient KB2P cells (IC50: 91 nmol/L) and BRCA2-proficient KP cells (IC50: 8,135 nmol/L) was observed for AZD2281 [3].

体内活性

Animals bearing SW620 xenografted tumors were treated with AZD2281 (10 mg/kg, po) in combination with TMZ (50 mg/kg, po) once daily for 5 consecutive days, after which the tumors were left to grow out. A considerable inhibition of tumor volumes as compared with that of the TMZ alone group was observed for the TMZ plus AZD2281 combinations [1]. Tumor volumes of control group mice increased during the experimental period. The tumor growth of cisplatin and AZD2281 (25 mg/kg/day, every three days for five treatments) groups significantly decreased compared to the control group, and that of combination group was further decreased [2]. Combination treatment of Calu-6 xenografts with olaparib and fractionated radiotherapy caused significant tumor regression relative to radiotherapy alone. Olaparib alone, when given as single or multiple daily doses, or in combination with fractionated radiotherapy, increased the perfusion of tumor blood vessels [4].

激酶实验

This assay determined the ability of test compounds to inhibit PARP-1 enzyme activity. The method that was used was as reported. We measured PARP-2 activity inhibition by using a variation of the PARP-1 assay in which PARP-2 protein (recombinant) was bound down by a PARP-2 specific antibody in a 96-well white-walled plate. PARP-2 activity was measured following 3H-NAD+ DNA additions. After washing, scintillant was added to measure 3 H-incorporated ribosylations. For tankyrase-1, an AlphaScreen assay was developed in which HIS-tagged recombinant TANK-1 protein was incubated with biotinylated NAD+ in a 384-well ProxiPlate assay. Alpha beads were added to bind the HIS and biotin tags to create a proximity signal, whereas the inhibition of TANK-1 activity was directly proportional to the loss of this signal. All experiments were repeated at least three times [1].

细胞实验

HSC-2, Ca9-22, and SAS oral carcinoma cells were seeded in 24-well plates at a density of 2 × 104 cells/well. After overnight incubation, the culture medium was replaced with fresh medium containing various concentrations of PARP inhibitor AZD228 or cisplatin. After 24 h of treatment, the number of viable cells was assessed using an MTT assay as reported previously. Briefly, one-tenth of the fluid volume of 5 mg/mL MTT in RPMI-1640 medium was added to each well, followed by incubation for 4 h at 37 °C. After incubation, the medium was carefully removed and an adequate volume of 0.1 N HCl in isopropanol was added to each well and the resultant formazan crystals was dissolved. Absorbance was determined at 570 nm by microplate reader in 96-well assay plates. All experiments were performed in triplicate [2].

细胞系: Breast cancer cell lines including SW620 colon, A2780 ovarian, HCC1937, Hs578T, MDA-MB-231, MDA-MB-436, and T47D

动物实验

Once the tumor diameter had reached 7 mm, the mice were randomly assigned to the following groups: (a) control (200 μL saline); (b) cisplatin (2 mg/kg per body weight, dissolved in 200 μL sterilized water); (c) AZD2281 (25 mg/kg per body weight, dissolved in 200 μL sterilized water); or (d) combination (both cisplatin and AZD2281). The chemicals were administered intraperitoneally every three days, five times. Although AZD2281 is administered orally in the clinic, intraperitoneal injection was recommended by the manufacturer because of easier manipulation and the ethical constraints associated with oral gavage administration to mice. Tumor size and body weight were measured at the time of administration. The tumor volume was calculated using following equation. Tumor volume = verticality × width × height × 0.5236 Three days after the last administration, all surviving mice were sacrificed [2].

动物模型:Brca1-/-;p53-/- mammary tumors are generated in K14cre;Brca1F/F;p53F/F mice.

化学信息

分子量

434.46

分子式

C24H23FN4O3

CAS

763113-22-0

溶解度

DMSO: 80 mg/mL (184.1 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 2.302 ml 11.509 ml 23.017 ml
5 mM 0.46 ml 2.302 ml 4.603 ml
10 mM 0.23 ml 1.151 ml 2.302 ml
50 mM 0.046 ml 0.23 ml 0.46 ml

参考文献
 
1. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91.
2. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272.
3. Evers B, et al. Selective inhibition of BRCA2-deficient mammary tumor cell growth by AZD2281 and cisplatin. Clin Cancer Res. 2008 Jun 15;14(12):3916-25.
4. Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58.
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