达卡他韦配合锭(Ximency Combination Tablets)说明书

产地国家:日本

处方药:是

所属类别: (16.5/15/100)毫克/片 56片/盒

包装规格: (16.5/15/100)毫克/片 56片/盒

计价单位:盒

生产厂家英文名:Bristol Myers Squibb Co.Ltd.

原产地英文商品名:Ximency Combination Tablets(ジメンシー配合錠)56tabs/box

原产地英文药品名:Daclataasvir Hydrochlorde/Asunaprevir/Beclabuvir Hydrochloride

中文参考商品译名:Ximency(ジメンシー配合錠)56片/盒

中文参考药品译名:Daclataasvir Hydrochlorde/Asunaprevir/Beclabuvir Hydrochloride

简介

近日,百时美施贵宝的新药Ximency在日本获批上市,用于治疗基因 1型慢性丙肝或代偿性丙型肝硬化患者的病毒血症的新药Ximency(daclatasvir hydrochloride/asunaprevir/beclabuvir hydrochloride三联方)在日本获批。

Ximency是3种直接作用的抗病毒药物的联方,包括NS5A复制复合物抑制剂daclatasvir;NS3/4蛋白酶抑制剂sunaprevir和新型的NS5B抑制剂beclabuvir hydrochloride。在日本进行的针对未经治疗或未经干扰素治疗过的基因 1型慢性丙肝或代偿性丙型肝硬化患者III期临床试验中,其主要临床重点,在12周内有95.9%的受试者表现出了持续的病毒学应答(SVR12,95%置信区间为90.8-98.7%),且其应答率与患者的背景(年龄、性别、纤维化等级、治疗历史、是否有补偿性肝硬化、IL28基因型等)和是否有NS5A-L31和Y93突变没有显著性差异。Ximency的主要副作用为谷丙转氨酶升高(23.0%),谷草转氨酶升高(19.4%),嗜酸粒细胞增多(17.1%),发热(16.6%)和高胆红素血症(14.7%)。ジメンシー配合锭药物分类名称抗病毒剂批准日期:2017年2月

欧文商标名:Ximency Combination Tabletsダクラタスビル塩酸塩

一般名:ダクラタスビル塩酸塩(Daclatasvir Hydrochloride)

化学名

Dimethyl N,N ’-([1,1’-biphenyl]-4,4’-diylbis{1H-imidazole-5,2-diyl-[(2S)-pyrrolidine-2,1-diyl][(1S)-3-methyl-1-oxobutane-1,2-diyl]})dicarbamate dihydrochloride分子式:C40H50N8O6・2HCl

分子量:811.80

性状:Daclatasville hydrochloride是一种白色至黄色粉末。 易溶于水或二甲基亚砜,微溶于乙醇(99.5)。アスナプレビル

一般名:アスナプレビル(Asunaprevir)

化学名

1,1-Dimethylethyl{(2S)-1-[(2S,4R)-4-({7-chloro-4-methoxyisoquinolin-1-yl}oxy)-2-({(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl}carbamoyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl}carbamate

分子式:C35H46ClN5O9S

分子量:748.29

性状:Asnaprevir是一种白色至微黄色的白色粉末。 它极易溶于乙腈或二甲基亚砜,微溶于乙醇(99.5),几乎不溶于水。ベクラブビル塩酸塩

一般名:ベクラブビル塩酸塩(Beclabuvir Hydrochloride)

化学名

(4bS,5aR)-12-Cyclohexyl-N-(dimethylsulfamoyl)-3-methoxy-5a-[(3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl)carbonyl]-4b,5,5a,6-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-9-carboxamide monohydrochloride

分子式:C36H45N5O5S・HCl

分子量:696.30

性状:Beclabville盐酸盐是白色至微黄色的白色粉末。 它易溶于N-甲基吡咯烷酮,微溶于水或乙醇(99.5)。批准条件制定药品风险管理计划并适当实施。在制造和销售之后累积一定数量的案例数据之前,通过针对所有用例案例进行使用结果调查,有必要掌握患者的背景信息, 收集有关安全性和有效性的数据,并采取必要措施正确使用该药物。

药用药理学

作用机制达卡他韦:它是构成HCV复制所必需的HCV复制复合物的多功能蛋白NS5A的抑制剂,并通过抑制NS5A蛋白的功能来抑制HCV复制。Asunaprevir:它是HCV复制所需的HCV NS3 / 4A蛋白酶复合物的抑制剂,并抑制HCV多蛋白加工,用于病毒复制所必需的成熟病毒蛋白质生产。Beklab Buil:它是HCV复制所必需的HCV NS5B RNA依赖性RNA聚合酶的非基于核酸的抑制剂,结合NS5B聚合酶拇指位点1并抑制RNA合成的起始。

抗病毒活性Daklatasville,asnaprevir和beclabville抑制不同的HCV蛋白(NS5A,NS3 / 4A蛋白酶和NS5B聚合酶)。在使用HCV复制子细胞的这些抑制剂的组合试验中观察到抗病毒活性的添加或协同作用。

达卡他韦:对于基因型1b和1a的HCV复制子,EC50值分别为0.001至0.009nmol / L和0.003至0.050nmol / L.Asunaprevir:对于基因型1b和1a的NS 3/4 A蛋白酶复合物,IC 50值分别为0.3nmol / L和0.7-1.8nmol / L.此外,对于基因型1b和1a的HCV复制子,EC50值为1.2nmol/L和4nmol/L被抑制。Beklab Buil:对于基因型1b和1a的NS5B聚合酶,IC50值分别为4.2nmol / L和3.3nmol / L.也显示出的EC 50的抑制效果值分别为3.5〜9.5nmol / L和1.6〜5.3nmol/L的HCV复制子基因型1b和1a。

耐药性在HCV复制子细胞测定,达卡他韦,但电阻Asunaprevir或Bekurabubiru,抗HCV效果的单一疗法应用被表示并标抗性发展的抑制是由这三种试剂的组合观察到的。达卡他韦:作为对Daclatasville产生抗性的HCV复制子细胞的基因分型的结果,在NS5A的氨基酸1至100中发现了多个取代。在基因型1b的情况下,在L31和Y93中经常观察到抗性替换。氨基酸取代的一个位置(例如Y93H),复制子的EC 50值引入这些取代是野生型小于30倍。此外,当在两个氨基酸(例如,L31V-Y93H)存在取代时,EC 50值是野生型的1000倍以上。Asunaprevir:作为对asnaprevir产生抗性的HCV复制子细胞的基因分型分析的结果,证实了用D168的A,G,H,V或Y取代NS3蛋白酶。引入这些取代的基因型1b复制子的EC 50值是野生型的16-280倍。Beklab Buil:作为对beclavir产生抗性的HCV复制子细胞的基因分型的结果,在NS5B聚合酶的P495中发现了取代。在基因型1b中,基因型1a,S,A,L中的S,A,L,T代替P495。引入这些取代的复制子的EC 50值是野生型的15至64倍。通常,复制子的复制效率与耐受程度成反比。交叉耐受达卡他韦,有抗药性的取代每个代理Asunaprevir或Bekurabubiru有具有序聚乙二醇化干扰素α和作用机理不同的抗HCV剂足够的灵敏度HCV复制子细胞[例如,NS5A的耐药性相关的变体对NS 3/4蛋白酶抑制剂和NS 5 B聚合酶抑制剂(核酸系统和非核酸系统)敏感]。

适应症

改善慢性丙型肝炎或C型肝硬化血清群1(基因型1)中的病毒血症

用法与用量

成人,在饭后每天两次服用2片,并且给药期为12周。

包装组合

56片(8片×7)PTP制造供应商Bristol-Myers Squibb Co.Ltd。

英文版说明书

Bristol-Myers Squibb acquires approval for manufacturing and marketing of “Dimency compound tablet” for treatment of chronic hepatitis CNotification of Acquisition of Manufacture and Marketing Approval for “Cosmetic (R) Combination Tablet”, a Treatment for C Type Chronic Hepatitis Combined with Three Direct Action Type Antiviral AgentsBristol-Myers Squibb Co., Ltd. (Shinjuku-ku, Tokyo, President and CEO: David Piras) today announced that it has incorporated three orthodontic antiviral agents (DAA) (Generic name: Daclatasville hydrochlorid/asnaprevir/beclabuv hydrochloride, below: jimency) for the improvement of viremia in serogroup 1 (genotype 1) chronic hepatitis C or C type compensatory cirrhosis , We will inform you that we have obtained manufacture and marketing approval from the Ministry of Health, Labor and Welfare.Jimensey blended beclabuv hydrochloride (hereinafter Beklabuville), a novel DAA, into Dunectasville hydrochloride, an NS5A replication complex inhibitor developed by Bristol-Myers Squibb, USA, and asnaprevir, an NS3/4A protease inhibitor It is a fixed dose combination.Beklabuville, a novel DAA, is a non-nucleic acid based inhibitor for nonstructural protein 5B (NS5B) polymerase. By adding beclavubil to Daclatususville and Asnaprevir with different points of action, suppression effect on additive/synergistic effect and tolerance development It is approved. It is Japan’s first as a formulation containing three different DAAs with different points of action.In domestic phase III trial, dosimetry was administered to genotype 1 type C chronic hepatitis C or type C compensated liver cirrhosis patients who were untreated and treated with interferon formulation in the domestic Phase III trial, and as a result, the main endpoint was untreated genotype 95% confidence interval (95% confidence interval: 90.8 to 98.7%) of SVR 12 in the jimmy group of chronic hepatitis C patients with type 1 b (HCV RNA at 12 weeks after administration is below the lower limit of quantification) did. In addition, the total of genotype 1a/1b chronic hepatitis C and compensated liver cirrhosis patients also showed 95.9%, and in subgroup analysis, age, gender, degree of fibrosis, prior treatment history, compensatory liver cirrhosis Excellent effectiveness was confirmed regardless of presence / absence, background factor such as IL28B genotype, presence or absence of resistance mutation of NS5A-L31 and Y93.The main side effects due to the dimen- sity were 23.0% increase in ALT (GPT), 19.4% increase in AST (GOT), 17.1% in eosinophilia, 16.6% in fever, high Bilirubinemia was 14.7% etc.In September 2014, we launched “Dacruinza (R) Tablets 60 mg” and “Sumbpa (R) Capsules 100 mg”, a treatment for chronic hepatitis C only by oral medicine which does not require interferon and ribavirin for the first time in Japan. We will continue to do our utmost to develop hope for patients and families with innovative medicines and strive to promote proper use of medicines.■ Product overview of Jimency·Product name: GENENCY (R) combination tablet·Generic name: Daclatasville hydrochloride/asnaprevir/ beclabville hydrochloride·Indication or effect: Improve viremia in serogroup 1 (genotype 1) in chronic hepatitis C or type C liver cirrhosis·Dosage regimen and dose: In adults, normally 2 tablets are administered orally twice a day after meals, and the administration period is 12 weeks·Ingredients·Content: 16.5 mg of Daclatasville hydrochloride (15 mg as Daclatasville) / 1 in Asprevir / 39.6 mg of Beclabville hydrochloride (37.5 mg in beclave) in 1 tablet· Manufacturing marketing approval acquisition date: December 19, 2016·Manufacturer selling agency: Bristol · Myers Squibb Co., Ltd.

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