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  药店国别: 德国药房
产地国家: 德国
所属类别: 抗癌药物->治疗卵巢癌药物
处方药:处方药
包装规格: 100毫克/胶囊 56胶囊/盒
计价单位:
  点击放大  
生产厂家英文名:
Tesaro Bio
该药品相关信息网址1:
https://www.zejula.com/en/why-zejula?gclid=Cj0KCQjwlK7cBRCnARIsAJiE3MjNaamNAVTsKqoqo19hZXFZ7mUs_BdOtF5-SIBpGoVbgaDc2SdTIGQaAvjXEALw_wcB
该药品相关信息网址2:
https://www.drugs.com/zejula.html
该药品相关信息网址3:
https://en.wikipedia.org/wiki/Niraparib
原产地英文商品名:
Zejula 100mg 56 capsules
原产地英文药品名:
Niraparib
中文参考商品译名:
Zejula 100毫克 56粒
原产地国家批准上市年份:
1979/08/02
英文适应病症1:
Ovarian cancer
英文适应病症2:
Breast cancer
临床试验期:
完成
中文适应病症参考翻译1:
卵巢癌
中文适应病症参考翻译2:
乳腺癌
药品信息:

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 详细处方信息以本药内容附件PDF文件(20189223491515.pdf)的“原文Priscribing Information”为准
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部分中文Zejula处方资料(仅供参考)

英文药名:Zejula Capsules

中文药名:尼拉帕尼胶囊

生产厂家:Tesaro

药品简介

2017年9月18日,Zejula(niraparib):由Tesaro公司开发,该药是一种口服多聚ADP核糖聚合酶(PARP)抑制剂,利用DNA修复途径的缺陷,优先杀死癌细胞。这种作用模式,赋予了niraparib治疗具有DNA修复缺陷的广泛肿瘤类型的潜力。PARP与广泛的肿瘤类型相关,尤其是乳腺癌和卵巢癌。 具体而言,CHMP推荐批准Zejula作为一种单药疗法,用于接受含铂化疗实现完全缓解或部分缓解的铂敏感复发性高级别浆液性上皮性卵巢、输卵管或原发性腹膜癌成人患者的治疗。如果获批,niraparib将成为欧洲首款也是唯一一款不用区分BRCA基因突变或生物标志物的PARP抑制剂。

【原研厂商】TESARO

【剂 型】胶囊

作用机制

Niraparib是一种聚(ADP-核糖)聚合酶(PARP)酶,PARP-1和PARP-2的抑制剂,它们在DNA修复中起作用。体外研究曽显示niraparib-诱导细胞毒性可能涉及PARP酶活性的抑制作用和增加PARP-DNA复合物的形成导致DNA损伤,凋亡和细胞死亡。在BRCA1/2有或无缺陷肿瘤细胞系中观察到增加niraparib-诱导的细胞毒性。在BRCA1/2有缺陷小鼠肿瘤细胞的异种移植模型和在人有同源重组有或突变或野生型BRCA1/2缺乏患者-衍生移植瘤模型Niraparib减低肿瘤生长。

适应证

ZEJULA是一种聚(ADP-核糖)聚合酶(PARP)抑制剂适用为有复发性表皮卵巢,输卵管,或原发性腹膜癌患者对基于铂化疗是一个完全或部分缓解成年患者的维持治疗。 剂量和给药方法

● 推荐剂量是300mg每天1次有或无食物服用.

● 继续治疗直至疾病进展或不可接受不良反应。

● 对不良反应,考虑中断治疗,剂量减低,或给药终止.

剂型和规格

胶囊:100mg

禁忌证

无。

警告和注意事项

● 骨髓增生异常综合征/急性髓性白血病(MDS/AML):暴露于ZEJULA患者发生MDS/AML,和有些病例是致敏性。监视患者对血液学毒性和终止如MDS/AML被确证

不良反应

最常见不良反应(发生率 ≥10%)是血小板减少,贫血,中性细胞减少,白细胞减少,心悸,恶心,便秘,呕吐,腹痛/腹胀,粘膜炎/胃炎,腹泻,消化不良,口干,疲劳/乏力,减低食欲,泌尿道感染,AST/ALT升高,肌痛,背痛,关节痛,头痛,眩晕,味觉障碍,失眠,焦虑,鼻咽炎,呼吸困难,咳嗽,皮疹,和低血压.

特殊人群中使用

● 哺乳:建议妇女治疗期间和接受最后给药后共1个月不要哺乳喂养。

产品特点:

PARP和BRCA是细胞内两种重要的DNA修复机制,前者主要修复DNA单链损伤,后者主要修复DNA双链损伤,双重守护细胞健康,保证细胞内DNA损伤得到及时修复而避免癌变。PARP和BRCA任一修复机制失灵,损伤DNA会在细胞内累积导致癌变,累积过度也会导致癌细胞死亡。

ADP核糖聚合酶(PARP)在DNA修复和转录调节过程中起作用。

niraparib(mk4827)是一种口服的选择性PARP -1和PARP -2抑制剂,IC50分别为3.8nM 和2.1nM。MK 4827抑制PARP活性的EC50为4nM,抑制BRCA-1和BRCA-2突变的肿瘤细胞增殖的CC50范围在10-100nM之间。在缺乏brca和pten功能的基础肿瘤模型中可诱导致死性变化的产生,能抑制细胞对DNA损伤的修复。对于带有BRCA基因突变的癌细胞来说,倘若PARP活性进一步受到抑制,这些细胞分裂时就会产生大量DNA损伤,导致癌细胞死亡。

有些人由于先天或后天原因,BRCA基因发生突变而失去活性,细胞内会因为损伤DNA累积导致癌症风险升高,特别是乳腺癌和卵巢癌风险。而BRCA突变型癌细胞由于BRCA失活,DNA损伤修复变得非常依赖于PARP,倘若PARP活性进一步受到抑制,这些细胞分裂时就会产生大量DNA损伤,导致癌细胞死亡。

尼拉帕尼与以往两类PARP抑制剂药物奥拉帕尼(olaparib)以及卢卡帕利(rucaparib)临床优势:

以往两类PARP抑制剂药物奥拉帕尼(olaparib)以及卢卡帕利(rucaparib)在批准时都需要患者具有BRCA基因的突变。而新上市的PARP抑制剂新药Niraparib试验结果给力,不仅在BRCA胚系突变的患者中表现出优势(21:5.5月),在无BRCA胚系突变的患者中也同样具有明显的生存优势(9.3:3.9月)。因而在FDA批准时并未要求患者一定要具有BRCA的突变,而只是提及铂类敏感,因为顺铂卡铂等铂类药物也是作用于DNA结构,对铂类药物的敏感性一定程度上反映了肿瘤细胞对DNA破坏类药物(如PARP抑制剂)的潜在敏感性,提高适用人群的筛选性,另外,铂类与PARP先后顺序也存在相互协同治疗作用。这意味着卵巢癌患者近期对铂类治疗敏感(达到PR以上)的患者都可以尝试使用Niraparib,适用患者人群范围大大增加。同时该药物主要口服用药,增加治疗便利。

English name: Zejula Capsules

 

Chinese medicine name: Nilapani capsule

Manufacturer: Tesaro

Introduction to Drugs

September 18, 2017, Zejula (niraparib): Developed by Tesaro, an oral poly ADP ribose polymerase (PARP) inhibitor that uses DNA repair pathway defects to preferentially kill cancer cells. This mode of action confers the potential of niraparib to treat a wide range of tumor types with DNA repair defects. PARP is associated with a wide range of tumor types, especially breast and ovarian cancer. Specifically, CHMP recommends the approval of Zejula as a monotherapy for platinum-sensitive recurrent high-grade serous epithelial ovarian, fallopian tube or primary peritoneal cancer in adults undergoing complete or partial remission with platinum-containing chemotherapy. treatment. If approved, niraparib will be the first and only PARP inhibitor in Europe that does not distinguish between BRCA mutations or biomarkers.

[Original researcher] TESARO

[Formulation] Capsule

Action mechanism

Niraparib is a poly(ADP-ribose) polymerase (PARP) enzyme, an inhibitor of PARP-1 and PARP-2, which plays a role in DNA repair. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzyme activity and increased formation of PARP-DNA complexes leading to DNA damage, apoptosis and cell death. Increased niraparib-induced cytotoxicity was observed in BRCA1/2 with or without defective tumor cell lines. A xenograft model of BRCA1/2 deficient mouse tumor cells and a human-derived or wild-type BRCA1/2 deficient patient-derived xenograft model Niraparib reduced tumor growth in humans.

Indications

ZEJULA is a poly(ADP-ribose) polymerase (PARP) inhibitor for patients with recurrent epidermal ovary, fallopian tube, or primary peritoneal cancer. Platinum-based chemotherapy is a maintenance therapy that completely or partially relieves adult patients. Dosage and method of administration

● The recommended dose is 300mg once daily with or without food.

● Continue treatment until disease progression or unacceptable adverse reactions.

● For adverse reactions, consider discontinuation of treatment, dose reduction, or termination of dosing.

Formulations and specifications

Capsule: 100mg

Contraindications

no.

Warnings and Precautions

● Myelodysplastic syndrome/ acute myeloid leukemia (MDS/AML): MDS/AML occurs in patients exposed to ZEJULA, and in some cases is allergenic. Surveillance of patients with hematological toxicity and termination as confirmed by MDS/AML

Adverse reactions

The most common adverse reactions (incidence ≥10%) are thrombocytopenia, anemia, neutropenia, leukopenia, palpitations, nausea, constipation, vomiting, abdominal pain/bloating, mucositis/gastritis, diarrhea, indigestion, dry mouth, Fatigue/weakness, reduced appetite, urinary tract infection, elevated AST/ALT, myalgia, back pain, joint pain, headache, dizziness, dysgeus, insomnia, anxiety, nasopharyngitis, difficulty breathing, cough, rash, and hypotension .

Use

in special people

● Breastfeeding: It is recommended that women should not breastfeed during the treatment period and for one month after receiving the final dose.

Product Features:

PARP and BRCA are two important DNA repair mechanisms in the cell. The former mainly repairs DNA single-strand damage, the latter mainly repairs DNA double-strand damage, and double protects cell health, ensuring timely repair of DNA damage in cells and avoiding cancer. Any repair mechanism of PARP and BRCA fails, and the damaged DNA will accumulate in the cells to cause cancer, and excessive accumulation will also lead to cancer cell death.

ADP ribose polymerase (PARP) plays a role in DNA repair and transcriptional regulation.

niraparib (mk4827) is an oral selective PARP-1 and PARP-2 inhibitor with IC50 of 3.8 nM and 2.1 nM, respectively. The EC50 of MK 4827 inhibiting PARP activity was 4 nM, and the CC50 of tumor cell proliferation inhibiting BRCA-1 and BRCA-2 mutations ranged from 10-100 nM. In the basal tumor model lacking brca and pten function, the production of lethal changes can be induced, which can inhibit the repair of DNA damage by cells. For cancer cells with BRCA gene mutations, if PARP activity is further inhibited, these cells will produce a large amount of DNA damage when they divide, leading to cancer cell death.

Some people lose their activity due to mutations in the BRCA gene due to congenital or acquired factors. The risk of cancer is increased in cells due to the accumulation of damaged DNA, especially breast cancer and ovarian cancer. While BRCA mutant cancer cells are inactivated due to BRCA, DNA damage repair becomes very dependent on PARP. If PARP activity is further inhibited, these cells will produce a large amount of DNA damage when they divide, leading to cancer cell death.

Nirapani and the two previous PARP inhibitors, olaparib and rucaparib, have clinical advantages:

In the past, two types of PARP inhibitor drugs, olaparib and rucaparib, required mutations in the BRCA gene when approved. The newly-released PARP inhibitor new drug Niraparib test results show that it not only shows superiority in patients with BRCA germline mutations (21:5.5 months), but also has obvious survival advantages in patients without BRCA germline mutations (9.3 :3.9 months). Therefore, the FDA approval does not require patients to have BRCA mutations, but only mention platinum-sensitive, because platinum drugs such as cisplatin and platinum also act on DNA structure, and the sensitivity to platinum drugs reflects to some extent. The potential sensitivity of tumor cells to DNA-destroying drugs (such as PARP inhibitors) improves the screening of the applicable population. In addition, there is a synergistic therapeutic effect between platinum and PARP. This means that patients with ovarian cancer who are sensitive to platinum therapy (above PR) can try Niraparib, and the range of patients is greatly increased. At the same time, the drug is mainly administered orally to increase the convenience of treatment.

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CONTRAINDICATIONS
A history of allergic reaction to any of the penicillins is a contraindication

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 详细处方信息以本药内容附件PDF文件(20189223491515.pdf)的“原文Priscribing Information”为准
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于2019年1月8日更新

更新日期: 2019-1-8
附件:
20189223491515.pdf    

 
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