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  药店国别: 日本药房
产地国家: 日本
所属类别: 急性疾病->流感
处方药:处方药
包装规格: 10毫克/片, 10片/盒
计价单位:
  点击放大  
生产厂家中文参考译名:
塩野義製薬株式会社
生产厂家英文名:
Shionogi & Co., Ltd.
该药品相关信息网址1:
https://iyakujoho.com/2018/03/14/hatsubai-xofluza/
该药品相关信息网址2:
https://en.wikipedia.org/wiki/Baloxavir_marboxil
原产地英文商品名:
XOFLUZA(ゾフルーザ錠)10mg/Tablets 10 Tablets/box
原产地英文药品名:
Baloxavir Marboxil
中文参考商品译名:
XOFLUZA(ゾフルーザ錠)10毫克/片 10片/盒
中文参考药品译名:
Baloxavir Marboxil
原产地国家批准上市年份:
2018/03/00
英文适应病症1:
Influenza A virus
英文适应病症2:
Influenza B virus
临床试验期:
完成
中文适应病症参考翻译1:
甲型流感病毒
中文适应病症参考翻译2:
乙型流感病毒
药品信息:

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 详细处方信息以本药内容附件PDF文件(201892421030024.pdf)的“原文Priscribing Information”为准
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部分XOFLUZA处方资料(仅供参考)

英文名:Baloxavir Marboxil

商标名:XOFLUZA

中文名:曾用名S-033188

生产商:盐野义制

药品简介

药物分类名称

抗流感病毒剂

批准日期:2018年3月

欧文商標名:XOFLUZA

一般的名称:バロキサビル マルボキシル(JAN)

Baloxavir Marboxil

化学名:({(12aR)-12-[(11S)-7,8-Difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-6,8-dioxo-3,4,6,8,12,12a-hexahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin-7-yl}oxy)methyl methyl carbonate

分子式:C27H23F2N3O7S

分子量:571.55

性状:

它是白色至浅黄白色粉末。

易溶于二甲基亚砜,微溶于乙腈,难溶于甲醇或乙醇(99.5),难溶于水。

熔点:约228°C(分解)

分配系数:log P = 2.26 [1-辛醇/水]

批准条件

制定药品风险管理计划并适当实施。

药用药理学

1.体外病毒生长抑制作用

在用A和B流感病毒的实验室菌株或临床分离株(包括显示对神经氨酸酶抑制剂的敏感性降低的NA / H274Y突变体)感染的MDCK细胞(源自犬肾的细胞系)中,valoxabile marboxyl 活性形式显示出病毒生长抑制作用。 [病毒滴度被抑制到1/10的浓度(EC 90)对于A型为0.46至0.98 nmol/L,对于B型为2.21至6.48 nmol/L.]

在感染H5N1或H7N9亚型禽流感病毒的MDCK细胞中也观察到这种效应(包括NA / H274Y,NA / R292K突变株对神经氨酸酶抑制剂的敏感性降低))。 (EC 90:0.80至3.16nmol / L)

2.体内抗病毒作用

与类型A和B型流感病毒实验室菌株或临床分离株接种的小鼠模型小鼠肺内病毒后(包括NA / H274Y突变体显示出降低的敏感性,以神经氨酸酶抑制剂),Barokisabiru Marubokishiru给药天滴度以剂量依赖性方式降低。用流感接种这种效果,模型14)在小鼠中病毒毒株抑制免疫功能,进一步,同样在禽流感病毒株(H5N1,H7N9)接种小鼠模型13)进行观察。

此外,与类型A和B型流感病毒株或禽流感病毒株(H5N1,H7N9)接种小鼠致死性模型中,Barokisabiru Marubokishiru提高死亡率。与接种流感病毒毒株的小鼠模型中,该治疗效果,14也观察到延迟处理开始(开始病毒接种后24至96小时施用))。 与接种流感病毒株雪貂模型,Barokisabiru Marubokishiru降低病毒滴度施用,在体温抑制增加第二天洗鼻。

3.作用机制

valoxabile marboxylic activator选择性地抑制A型和B型流感病毒的帽依赖性内切核酸酶活性。 帽依赖性内切核酸酶是特异性切割宿主细胞衍生的mRNA前体的酶,并产生RNA片段,其是病毒mRNA合成所必需的引物。 valoxabile羧酸活化剂通过抑制帽依赖性内切核酸酶活性和抑制病毒mRNA的合成而发挥病毒生长抑制作用。

4.抵抗

在III期临床试验的国内针对儿童超过12岁以下,在患者用此药已经施用,77例患者中18例患者核苷酸序列分析给药前后(可能是要么A型流感病毒感染例)在聚合酶酸性蛋白区中的I38氨基酸突变为结合靶位点观察Barokisabiru Marubokishiru活性物质。在成人和12岁以上儿童的国际合作III期临床试验中,患者用此药已被给予370案件移出36案件序列分析之前和管理(A流感病毒后有可能传染性患者)接受氨基酸突变I38,其中在合并感染的患者一例A类和B型流感病毒时,观察到在这两种类型的I38的氨基酸变异。在任何的临床试验,在该药物的患者群中检测的氨基酸突变I38,采用在从该药物的给药3天观察到病毒效价的瞬时增加。顺便提及,在氨基酸突变的病毒滴度的变化存在的国际联合III期临床试验I38,在成人治疗的患者中观察到这种药物,并在图5中示出年龄大于12岁的儿童这是。

适应症

甲型流感或乙型流感病毒

用法与用量

1.对于12岁及以上的成人和儿童,以单剂量口服给予2mg 20mg片剂(40mg作为valoxabile maloxil)。 然而,对于体重为80千克或以上的患者,应口服一次4或20毫克片剂(80毫克,如valoxabile maloxil)。

2.对于12岁以下的儿童,以下剂量应按如下方式口服给药。

English name: Baloxavir Marboxil

Trademark name: XOFLUZA

Chinese name: used name S-033188

Manufacturer: Yan Yeyi System

Introduction to Drugs

Drug classification name

Anti-influenza virus

Approval date: March 2018

Owen trademark name: XOFLUZA

General name: バロキサビル マルボキシル (JAN)

Baloxavir Marboxil

Chemical name: ({(12aR)-12-[(11S)-7,8-Difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-6,8-dioxo-3, 4,6,8,12,12a-hexahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin-7-yl}oxy) Methyl methyl carbonate

Molecular formula: C27H23F2N3O7S

Molecular weight: 571.55

trait:

It is a white to pale yellowish white powder.

Soluble in dimethyl sulfoxide, slightly soluble in acetonitrile, insoluble in methanol or ethanol (99.5), insoluble in water.

Melting point: about 228 ° C (decomposition)

Distribution factor: log P = 2.26 [1-octanol/water]

Approval Conditions

Develop a drug risk management plan and implement it appropriately.

Pharmacology & Pharmacology

1. In vitro virus growth inhibition

MDCK cells (cell lines derived from canine kidney) infected with laboratory strains or clinical isolates of influenza A and B viruses (including NA/H274Y mutants showing reduced sensitivity to neuraminidase inhibitors) The valoxabile marboxyl active form shows viral growth inhibition. [The concentration of virus titer suppressed to 1/10 (EC 90) is 0.46 to 0.98 nmol/L for type A and 2.21 to 6.48 nmol/L for type B.]

This effect was also observed in MDCK cells infected with H5N1 or H7N9 subtype avian influenza virus (including NA / H274Y, decreased sensitivity of the NA / R292K mutant to neuraminidase inhibitors)). (EC 90: 0.80 to 3.16 nmol / L)

2. Antiviral effect in vivo

Intrapulmonary virus in mice with mouse models of type A and B influenza virus isolates or clinical isolates (including NA/H274Y mutants showing reduced sensitivity to neuraminidase inhibitors) ), Barokisabiru Marubokishiru dosing titers decreased in a dose-dependent manner. This effect was inoculated with influenza, model 14) Inhibition of immune function by virus strains in mice, and further, observation in a mouse model of avian influenza virus strain (H5N1, H7N9) 13).

In addition, Barokisabiru Marubokishiru increased mortality in a mouse lethal model with type A and B influenza virus strains or avian influenza virus strains (H5N1, H7N9). In a mouse model inoculated with an influenza virus strain, this therapeutic effect, 14 was also observed to start the delayed treatment (administration 24 to 96 hours after the start of virus inoculation)). With the vaccination model of the influenza virus strain, Barokisabiru Marubokishiru reduced the virus titer application, and the nasal wash was increased the next day after the increase in body temperature.

3. Mechanism of action

Valoxabile marboxylic activator selectively inhibits cap-dependent endonuclease activity of influenza A and B viruses. A cap-dependent endonuclease is an enzyme that specifically cleaves a host cell-derived mRNA precursor and produces an RNA fragment that is a primer necessary for viral mRNA synthesis. Valoxabile carboxylic acid activators exert viral growth inhibition by inhibiting cap-dependent endonuclease activity and inhibiting viral mRNA synthesis.

4. Resistance

In the phase III clinical trials for children over 12 years of age, the patient has been administered this drug, and 18 of the 77 patients were enrolled before and after nucleotide sequence analysis (possibly either influenza A virus infection) The I38 amino acid mutation in the acidic region of the enzyme was observed to bind to the target site to observe the Barokisabiru Marubokishiru active substance. In the Phase III clinical trial of international cooperation between adults and children over 12 years of age, patients with this drug have been given 370 cases removed from the 36 case sequence analysis and managed (A flu virus may be infectious patients) to receive amino acid mutation I38, Amino acid variation in both types of I38 was observed in a case of influenza A and B viruses in patients with co-infection. In any clinical trial, the amino acid mutation I38 detected in the patient population of the drug was observed to have a transient increase in viral titer observed over 3 days from administration of the drug. Incidentally, in the International Joint Phase III Clinical Trial I38 in which the change in the viral titer of the amino acid mutation exists, this drug is observed in the adult-treated patient, and FIG. 5 shows the child older than 12 years old. .

Indications

Influenza A or Influenza B

Usage and usage

1. For adults and children 12 years of age and older, 2 mg of 20 mg tablets (40 mg as valoxabile maloxil) are administered orally in a single dose. However, for patients weighing 80 kg or more, 4 or 20 mg tablets (80 mg, such as valoxabile maloxil) should be taken orally once.

2. For children under 12 years of age, the following doses should be administered orally as follows.

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 详细处方信息以本药内容附件PDF文件(201892421030024.pdf)的“原文Priscribing Information”为准
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更新日期: 2018-10-03
附件:
201892421030024.pdf    

 
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