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波普瑞韦胶囊

新药编辑:新特药 更新时间:2015-02-04

  美国FDA于2011年5月13日批准Victrelis (boceprevir)与聚乙二醇干扰素α(peginterferon alfa)和利巴韦林(ribavirin)联用治疗成人慢性丙型肝炎。Victrelis适用于那些仍有部分肝功能且之前未曾接受过药物治疗或药物治疗无效的丙肝患者。
  4月27日FDA下属的抗病毒药专家咨询委员会以18比0的票数表决支持批准Victrelis。据悉,这是20年来FDA批准的第一种治疗丙肝新药。
  Victrelis的安全性与有效经过两项共1500名成年丙肝患者参加的3期临床试验得到验证。在两项试验中,与进行常规治疗(只服用聚乙二醇干扰素和利巴韦林)的患者相比,服用Victrelis(与聚乙二醇化干扰素和利巴韦林联合用药)的患者中有三分之二出现生显著增强的持续性病毒学反应(即停药24周后血液中检测不到丙型肝炎病毒)。
  持续病毒学反应可以降低肝硬化及其他肝病并发症、降低肝癌发病率和死亡率。如果病人结束治疗后其病毒学反应持续,则表明丙肝病毒感染已经被治愈。
  FDA相关主管官员表示,对于广大丙肝患者来说Victrelis是一个重大进展,与现有治疗药物相比,Victrelis为治疗丙肝这一严重疾病提供一个有效方法,为治愈丙肝带来了希望。
  据美国疾病预防控制中心统计,全美国共有320万人患有丙型肝炎。大多数肝炎患者一开始并无相关症状,一般几年后肝脏受损,症状随之出现。
  有美国,大多数肝移植都是因为丙型肝炎引起的相关肝病所致。感染丙肝病毒之后,大多数患者会发展成为慢性丙型肝炎,有些患者会在多年后发展成肝硬化,肝硬化会导致相关的肝病并发症,如出血、黄疸、腹腔积液、感染或肝癌等。
  感染丙肝病毒的途径有多种,主要包括:接触受丙肝病毒感染的血液、母婴传播、共用注射针头、性传播、与丙肝病人共用个人用品(如剃须刀、牙刷等)、未消毒纹身或穿刺器具等。
  Victrelis属于蛋白酶抑制剂类药物,其作用机制是附着于病毒阻止其复制繁殖。Victrelis为丸剂,1日3次,进餐时服用。
  Victrelis(与聚乙二醇干扰素和利巴韦林联用)常见的副作用包括困倦、低红细胞计数(贫血)、恶心、头痛和味觉障碍等。Victrelis由位于新泽西州的默克公司销售。
  另外,美国FDA于5月23日又批准了Vertex制药公司的Incivek(telaprevir)治疗丙型肝炎。
  VICTRELIS? (boceprevir)胶囊
  批准日期: 2011年5月13日;生产公司:Merck
  一般描述
  VICTRELIS(boceprevir)是丙型肝炎病毒(HCV)非-结构蛋白3(NS3)丝氨酸蛋白酶的一种抑制剂。
  Boceprevir有以下化学名:(1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3azabicyclo[3.1.0]hexan-2(S)-carboxamide. 分子式是C27H45N5O5和分子量是519.7。Boceprevir有以下结构式:
  Boceprevir是由两个非镜像异构体的接近等同混合物制造。Boceprevir是一种白色至淡白色无定形粉。自由溶于甲醇,乙醇和异丙醇和略溶于水。
  可得到为硬明胶胶囊为口服给药的VICTRELIS 200 mg胶囊。每个胶囊含200 mg  boceprevir和下列无活性成分:十二烷基硫酸钠,微晶纤维素,乳糖一水合物,交联羧甲基纤维素钠,预糊化淀粉[pre-gelatinized starch],和硬脂酸镁。红色胶囊由明胶,二氧化钛,D&C黄#10,FD&C蓝#1,和FD&C红#40。黄胶囊体含明胶,二氧化钛,D&C黄#10,FD&C红#40,和FD&C黄#6。胶囊用红和黄墨水印。红墨水含虫胶和红氧化铁,而黄墨水由虫胶,二氧化钛,聚乙烯吡啶酮和D&C黄#10铝色淀组成。.
  作用机制
  VICTRELIS是一种针对丙型肝炎病毒的直接作用抗病毒药[见微生物学(12.4)]。
  适应证和用途
  VICTRELIS是一种丙型肝炎病毒(HCV)NS3/4A蛋白酶抑制剂适用于与聚乙二醇干扰素α和利巴韦林[ribavirin]联用基因型1感染慢性丙型肝炎CHC)的治疗,在有代偿性肝病(≥18岁)成年患者,包括肝硬变,既往未治疗或既往干扰素和利巴韦林治疗已失败患者。(1)
  VICTRELIS必须不作为单药治疗使用。 (1)
  剂量和给药方法
  800 mg 每天口服三次给药(每7-9小时)与食物(一餐或小吃). (2)
  (1)VICTRELIS必须与聚乙二醇干扰素α和利巴韦林联用给药。 (2)
  (2)为特殊给药指导参考聚乙二醇干扰素α和利巴韦林包装插件。 (2)
  剂型和规格
  胶囊:200 mg(3)
  禁忌证
  (1)因为VICTRELIS必须与聚乙二醇干扰素α和利巴韦林给药,也应用对聚乙二醇干扰素α和利巴韦林所有禁忌证。 (4)
  (2)因为利巴韦林可能致出生缺陷和胎儿死亡,妊娠妇女中和女性伴侣妊娠男性禁忌boceprevir与聚乙二醇干扰素α和利巴韦林联用。(4)
  (3)与高度依赖CYP3A4/5清除的药物共同给药,和因为升高血浆浓度伴随严重和/或危及生命事件。 (4)
  (4)强CYP3A4/5诱导剂where显著减低boceprevir血浆浓度可能伴随减低疗效。 (4)
  警告和注意事项
  VICTRELIS与利巴韦林和聚乙二醇干扰素α使用:
  (1)利巴韦林可能致出生缺陷和胎儿死亡:在女性患者和男性患者的女性伴侣中避免妊娠。治疗前患者必须有妊娠检验阴性;使用两种或更多方式避孕,和每月妊娠检验。(5.1)
  (2)贫血 –VICTRELIS增添至聚乙二醇干扰素α和利巴韦林与单独聚乙二醇干扰素α和利巴韦林比较是伴随另外的血红蛋白浓度减低。(5.2)
  (3)中性粒细胞减少 - VICTRELIS增添至聚乙二醇干扰素α和利巴韦林可能导致伴随单独聚乙二醇干扰素α和利巴韦林治疗中性粒细胞减少恶化。(5.3)
  不良反应
  在临床试验中接受VICTRELIS与PegIntron和REBETOL联用成年受试者中最常报道的不良反应(大于35%受试者)是疲乏,贫血,恶心,头痛和味觉障碍。(6.1)
  为报告怀疑不良反应,联系Schering Corporation,Merck & Co., Inc.的子公司电话1-877-888-4231或FDA电话1-800-FDA-1088或www.fda.gov/medwatch.
  药物相互作用
  (1)VICTRELIS是一种CYP3A4/5强抑制剂和部分被CYP3A4/5代谢。治疗前和期间必须考虑药物-药物相互作用潜在可能。(4, 7, 12.3)
  特殊人群中使用
  (1)肝硬变:尚未在有代偿肝硬变患者或有一种器官移植患者中研究安全性和疗效。(8.7, 8.10)
  (2)与人类免疫缺陷病毒(HIV)合并感染:尚未确定有HCV和HIV合并感染患者中安全性和疗效。(8.8)
  (3)与乙型肝炎病毒(HBV)合并感染:尚未有HCV和HBV合并感染患者中研究安全性和疗效。(8.9)
  (4)儿童:尚未在儿童患者中研究安全性和疗效。(8.4)
  (5)可得到利巴韦林妊娠注册。 (8.1)
  如何供应/贮存和处置
  如何供应
  VICTRELIS 200 mg胶囊由红色帽与黄墨水印Merck标志,和黄色体部用红墨水印有“314” 组成。胶囊被包装在有28含12胶囊瓶的纸箱(NDC 0085-0314-02).
  贮藏和处置
  VICTRELIS 胶囊应贮存在冰箱2-8°C(36-46°F)直至发放。避免暴露于过热。对使用患者,冰箱贮存VICTRELIS胶囊可保持稳定至标签上失效期。VICTRELIS也可贮存在室温至25°C(77°F) 3个月。保持容器密闭。

  The FDA has approved Merck’s hepatitis C drug Victrelis, the first oral treatment for the disease.
  Victrelis (boceprevir) has been licensed to treat hepatitis C genotype 1 infection, in combination with current treatments peginterferon alfa (Roche’s Pegasys) and ribavirin.
  ABOUT VICTRELIS? (boceprevir)
  VICTRELIS is a prescription medicine used with the medicines peginterferon alfa and ribavirin (peg/riba) to treat long-lasting (chronic) hepatitis C genotype 1 infection in adults with stable (compensated) liver disease who have not been treated before or who have failed previous treatment. Do not take VICTRELIS alone. It is not known if VICTRELIS is safe and effective in children under 18 years of age.
  IMPORTANT SAFETY INFORMATION ABOUT VICTRELIS
  VICTRELIS plus peg/riba may cause birth defects or death of your unborn baby. If you are pregnant or your sexual partner is pregnant or plans to become pregnant, do not take these medicines.
  Females and males must use 2 forms of birth control during treatment and for 6 months after treatment with VICTRELIS plus peg/riba. Hormonal forms of birth control, such as birth control pills, vaginal rings, implants and injections, may not work as well during treatment with VICTRELIS and you may become pregnant.
  Females must have a pregnancy test before starting treatment with VICTRELIS plus peg/riba, every month while being treated, and every month for 6 months after all treatment is over.
  Read more Important Safety Information below
  Eligible patients may save on their out-of-pocket cost on up to 12 qualifying prescriptions of VICTRELIS. The coupon savings is valid for the eligible patient's co-pay, co-insurance or other out-of-pocket costs, up to a maximum benefit of 20% of the catalog price of VICTRELIS (as set by the manufacturer at the time of purchase), provided that coupon savings may not exceed the patient's actual out-of-pocket cost.
  VICTRELIS is a prescription medication. Only your health care provider can decide if VICTRELIS is right for you.
  ------------------------------------------------------------------------------------
  Indications:
  Chronic hepatitis C genotype 1 infection, in combination with peginterferon alfa and ribavirin in adult patients with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy. Not for use as monotherapy.
  Adult Dose:
  ≥18yrs: Take with food. 800mg three times daily. Start after 4 weeks therapy with peginterferon and ribavirin. Without cirrhosis: continue treatment as indicated by HCV-RNA levels at Weeks 8, 12, and 24 (see literature). With cirrhosis: continue for 44 weeks. Do not reduce dose. Discontinue if HCV-RNA levels indicate futility (see literature).
  Children's Dose:
  <18yrs: not recommended.
  Pharmacological Class:
  HCV NS3/4A protease inhibitor.
  Contraindications:
  Concomitant potent CYP3A4/5 inducers (eg, carbamazepine, phenobarbital, phenytoin, rifampin, St. John's Wort) or narrow therapeutic index CYP3A4/5 substrates (eg, alfuzosin, cisapride, ergot derivatives, lovastatin, simvastatin, drosperinone, pimozide, sildenafil or tadalafil for PAH, triazolam, oral midazolam). Pregnant women and men whose partners are pregnant (note: ribavirin is Cat. X). Review peginterferon and ribavirin contraindications.
  Warnings/Precautions:
  Female patients and partners must have (–) pregnancy test before therapy, use appropriate effective contraception, and undergo monthly pregnancy test. Monitor CBC w. differential, HCV-RNA. Co-infection with HBV or HIV. Decompensated cirrhosis. Organ transplant recipients. Pregnancy (Cat. B). Nursing mothers: not recommended.
  Interactions:
  See literature. Concomitant rifabutin, salmeterol, efavirenz, concomitant colchicine in renal or hepatic impairment: not recommended. Potentiates CYP3A4/5 substrates (eg, amiodarone, bepridil, propafenone, quinidine, flecainide, trazodone, desipramine, azole antifungals, clarithromycin). Antagonizes ethinyl estradiol. Antagonized by potent CYP3A4/5 inhibitors. Monitor warfarin, digoxin, dihydropyridine calcium channel blockers, bosentan, protease inhibitors, immunosuppressants, opioids. Concomitant ketoconazole, itraconazole: max 200mg/day. Concomitant atorvastatin: max 20mg/day. Colchicine, PDE5 inhibitors for ED (eg, sildenafil, tadalafil, vardenafil), alprazolam, IV midazolam: reduce doses and monitor. Corticosteroids: avoid, monitor if needed.
  Adverse Reactions:
  Fatigue, nausea, headache, dysgeusia, worsening anemia, neutropenia.
  ----------------------------------------------------------
  产地国家: 美国
  原产地英文商品名:
  VICTRELIS 200mg/cap 336caps
  原产地英文药品名:
  BOCEPREVIR
  中文参考商品译名:
  VICTRELIS 200毫克/胶囊 336胶囊
  中文参考药品译名:
  BOCEPREVIR
  生产厂家中文参考译名:
  先灵
  生产厂家英文名:
  SCHERING

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