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美国食品和药品监督管理局FDA2011年5月13日批准(boceprevir)治疗某些有慢性丙型肝炎成年。Victrelis 用于仍有某些肝功能，和who或既往未曾用药物治疗过其丙型肝炎或这类治疗已失败患者。
Victrelis被批准与聚乙二醇干扰素α和利巴韦林[ribavirin]联用
.
在两项有1,500例成年患者的3期临床试验中评价Victrelis的安全性和有效性。在两项试验中，2/3患者接受Victrelis与单独聚乙二醇化干扰素和利巴韦林联用与当前标准医治单独聚乙二醇化干扰素和利巴韦林比较，经历显著持续增加病毒学反应(即，停止治疗后24周血中再也检测不到丙型肝炎病毒)。
完成治疗后当一人持续病毒学反应，这提示 HCV感染已被治愈。持续病毒学反应可导致肝硬变和肝脏合并症减少, 肝癌(肝细胞癌)发生率减低，和死亡率减低。
FDA的药物评价和研究中心抗微生物产品室主任Edward Cox, M.D., M.P.H说：“对有丙型肝炎患者Victrelis是一个重要进展，”“这个新药对一个严重疾病提供一种有效治疗，和与当前可得到治疗比较提供更大机会治愈某些患者的丙型肝炎感染。”
按照美国疾病控制和预防中心,在美国有慢性丙型肝炎约3.2百万人，一种肝脏炎症引起病毒疾病可能导致肝功能减低或肝衰竭。
大多数有肝炎人们没有疾病症状直至发生肝损伤，可能经历数年。在美国进行肝移植大多数由于丙型肝炎病毒感染所致进行性肝病。丙型肝炎病毒(HCV)初始感染后，大多数人发生慢性丙型肝炎。有些经历许多年将发生肝硬变。肝硬变可能导致有合并症肝损伤，例如出血，黄疸(眼或皮肤发黄)，腹腔内积液，感染，或肝癌。
人们可能通过几种途径获得丙型肝炎病毒，包括：暴露于感染病毒的血液；有HCV母亲出生；共享针头；与感染人们性行为；与感染病毒人们共享个人用品如剃刀，牙刷，或来自未经消毒的纹身或穿刺工具。
Victrelis是药丸与食物服用每天3次。治疗是被称为蛋白酶抑制剂一类药物的一部分，其作用是与病毒结合和预防病毒倍增。
接受Victrelis与聚乙二醇化干扰素和利巴韦林联用患者最常报道的副作用包括疲乏，红细胞计数低(贫血)，恶心，头痛和味觉扭曲(味觉障碍)。
处方资料
VICTRELIS™ (boceprevir) 胶囊
美国初始批准：2011 优先审评药物
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。
VICTRELIS必须作为单药治疗使用。
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）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。
剂型和规格
胶囊：200 mg
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。
（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）强CYP3A4/5诱导剂where显著减低boceprevir血浆浓度可能伴随减低疗效。
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。
（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。
（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。
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。
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。
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。
（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。
（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。
（4）儿童：尚未在儿童患者中研究安全性和疗效。
（5）可得到利巴韦林妊娠注册。
Victrelis
Generic Name: boceprevir
Date of Approval: May 13, 2011
Company: Merck
Treatment for: Chronic Hepatitis C
FDA Approves Victrelis
The U.S. Food and Drug Administration (FDA) has approved Victrelis (boceprevir) for the treatment of chronic hepatitis C (CHC). Victrelis is approved for the treatment of CHC genotype 1 infection, in combination with peginterferon alfa and ribavirin, in adult patients (18 years of age and older) with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy.
Victrelis Medication Guide
Read this Medication Guide before you start taking Victrelis, and each time you get a refill. There may be important new information. This information does not take the place of talking with your doctor, nurse or physician assistant (healthcare provider) about your medical condition or your care.
Victrelis is taken along with peginterferon alfa and ribavirin. You should also read those Medication Guides.
Important information about Victrelis
Victrelis, in combination with peginterferon alfa and ribavirin, 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. You or your sexual partner should not become pregnant while taking Victrelis, peginterferon alfa, and ribavirin combination therapy and for 6 months after treatment is over.
•Females and males must use 2 forms of birth control during treatment and for 6 months after treatment with Victrelis, peginterferon alfa, and ribavirin. Hormonal forms of birth control, such as birth control pills, vaginal rings, implants and injections, may not work as well during treatment with Victrelis. You may get pregnant while using these birth control methods while on Victrelis. Talk to your healthcare provider about other forms of birth control that may be used during this time.
•Females must have a pregnancy test before starting treatment with Victrelis combination therapy, every month while being treated, and every month for 6 months after treatment with Victrelis, peginterferon alfa, and ribavirin is over.
•If you or your female sexual partner becomes pregnant while taking Victrelis, peginterferon alfa, and ribavirin or within 6 months after you stop taking these medicines, tell your healthcare provider right away. The Ribavirin Pregnancy Registry collects information about what happens to mothers and their babies if the mother takes ribavirin while she is pregnant.
•Do not take Victrelis alone to treat chronic hepatitis C infection. Victrelis must be used with peginterferon alfa and ribavirin to treat chronic hepatitis C infection.
What is Victrelis?
Victrelis is a prescription medicine used with the medicines peginterferon alfa and ribavirin to treat chronic (long-lasting) hepatitis C infection in adults who have not been treated before or who have failed previous treatment.
It is not known if Victrelis is safe and effective in children under 18 years of age.
Who should not take Victrelis?
See Important information about Victrelis
Do not take Victrelis if you:
•take certain medicines. Victrelis may cause serious side effects when taken with certain medicines. Read the section Before taking Victrelis.
Talk to your healthcare provider before taking Victrelis if you have any of the conditions listed below.
Before taking Victrelis
Before you take Victrelis, tell your healthcare provider if you:
•have certain blood disorders such as anemia (low red blood cell count).
•have liver problems other than hepatitis C infection.
•have human immunodeficiency virus (HIV) or any other immunity problems.
•have had an organ transplant.
•plan to have surgery.
•have any other medical condition.
•are breastfeeding. It is not known if Victrelis passes into breast milk. You and your healthcare provider should decide if you will take Victrelis or breastfeed. You should not do both.
Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.
Victrelis and other medicines may affect each other, causing side effects or affecting the way Victrelis and your other medicines work. Do not start taking a new medicine without telling your healthcare provider or pharmacist.
Do not take Victrelis if you take:
•alfuzosin hydrochloride (Uroxatral)
•anti-seizure medicines:
◦carbamazepine (Carbatrol, Epitol, Equetro, Tegretol, Tegretol XR, Teril)
◦phenobarbital
◦phenytoin (Dilantin)
•cisapride (Propulsid)
•drosperinone-containing medicines, including:
◦Yaz, Yasmin, Zarah, Ocella, Gianvi, Beyaz, Safyral
•ergot-containing medicines, including:
◦dihydroergotamine mesylate (D.H.E. 45, Migranal)
◦ergonovine and methylergonovine (Ergotrate, Methergine)
◦ergotamine tartrate (Cafergot, Migergot, Ergomar, Ergostat, Medihaler Ergotamine, Wigraine, Wigrettes)
•lovastatin (Advicor, Altoprev, Mevacor)
•midazolam (Versed), when taken by mouth
•pimozide (Orap)
•rifampin (Rifadin, Rifamate, Rifater, Rimactane)
•sildenafil (Revatio), when used for treating lung problems
•simvastatin (Simcor, Vytorin, Zocor)
•St. John's Wort (Hypericum perforatum) or products containing St. John's Wort
•tadalafil (Adcirca), when used for treating lung problems
•triazolam (Halcion)
Tell your healthcare provider if you are taking or starting to take any of these medicines:
•clarithromycin (Biaxin, Biaxin XL, Prevpac)
•dexamethasone
•efavirenz (Sustiva, Atripla)
•itraconazole (Sporanox)
•ketoconazole (Nizoral)
•posaconazole (Noxafil)
•rifabutin (Mycobutin)
•ritonavir (Norvir, Kaletra)
•voriconazole (Vfend)
Your healthcare provider may need to monitor your therapy more closely if you take Victrelis with the following medicines. Talk to your doctor if you are taking or starting to take these medicines:
•alprazolam (Xanax)
•amiodarone (Cordarone, Exterone, Pacerone)
•atorvastatin (Lipitor)
•bepridil (Vascor)
•bosentan (Tracleer)
•budesonide (Pulmicort, Pulmicort Flexihaler, Rhinocort, Pulmicort Respules, Symbicort)
•buprenorphine (Butrans, Buprenex, Suboxone, Subutex)
•cyclosporine (Gengraf, Neoral, Sandimmune)
•desipramine (Norpramin)
•digoxin (Lanoxin)
•felodipine (Plendil)
•flecainide (Tambocor)
•fluticasone (Veramyst, Flovent HFA, Flovent Diskus, Advair HFA, Advair Diskus)
•hormonal forms of birth control, including birth control pills, vaginal rings, implants and injections
•methadone (Dolophine)
•nifedipine (Procardia, Adalat CC, Procardia XL, Afeditab CR)
•nicardipine (Cardene SR, Cardene)
•propafenone (Rhythmol, Rhythmol SR)
•quinidine
•salmeterol (Advair HFA, Advair Diskus, Serevent)
•sirolimus (Rapamune)
•tacrolimus (Prograf)
•voriconazole (Vfend)
•colchicine (Colcrys, Probenecid and Colchicine, Col-Probenecid)
•trazadone (Desyrel)
•vardenafil (Staxyn, Levitra)
•warfarin (Coumarin)
How should I take Victrelis?
•Take Victrelis exactly as your healthcare provider tells you. Your healthcare provider will tell you how much to take and when to take it.
•Take Victrelis with food (a meal or light snack).
•Victrelis is packaged into single daily-use bottles. Each bottle has your entire day's worth of medicine. Make sure you are taking the correct amount of medicine each time.
•If you miss a dose of Victrelis and it is less than 2 hours before the next dose, the missed dose should be skipped.
•If you miss a dose of Victrelis and it is more than 2 hours before the next dose, take the missed dose with food. Take your next dose at your normal time and continue the normal dosing schedule. Do not double the next dose. If you have questions about what to do, call your healthcare provider.
•Your healthcare provider should do blood tests before you start treatment, at weeks 4, 8, 12, and 24, and at other times as needed during treatment, to see how well the medicines are working and to check for side effects.
•If you take too much Victrelis, call your healthcare provider or go to the nearest hospital emergency room right away.
Victrelis side effects
Victrelis may cause serious side effects, including:
See Important information about Victrelis
•Blood problems. Victrelis can affect your bone marrow and cause low red blood cell, and low white blood cell, counts. In some people, these blood counts may fall to dangerously low levels. If your blood cell counts become very low, you can get anemia or infections.
The most common side effects of Victrelis in combination with peginterferon alfa and ribavirin include:
•tiredness
•nausea
•headache
•change in taste
Tell your healthcare provider about any side effect that bothers you or that does not go away.
These are not all the possible side effects of Victrelis. For more information, ask your healthcare provider or pharmacist.
How should I store Victrelis?
•Store Victrelis capsules in a refrigerator at 36°-46°F (2-8°C). Safely throw away refrigerated Victrelis after the expiration date.
•Victrelis capsules may also be stored at room temperature up to 77°F (25°C) for 3 months.
•Keep Victrelis in a tightly closed container and away from heat.
Keep Victrelis and all medicines out of the reach of children.
General Information About the Safe and Effective Use oF Victrelis
Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide.
Do not use Victrelis for a condition for which it was not prescribed. Do not give Victrelis to other people, even if they have the same symptoms that you have. It may harm them.
This Medication Guide summarizes the most important information about Victrelis. If you would like more information, talk with your healthcare provider. You can ask your pharmacist or healthcare provider for information about Victrelis that is written for health professionals.
What are the ingredients in Victrelis?
Active ingredients: boceprevir
Inactive ingredients: sodium lauryl sulfate, microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, pre-gelatinized starch, and magnesium stearate.
Red capsule shell: gelatin, titanium dioxide, D&C Yellow #10, FD&C Blue #1, FD&C Red #40.
Yellow capsule shell: gelatin, titanium dioxide, D&C Yellow #10, FD&C Red #40, FD&C Yellow #6.
Red printing ink: shellac, red iron oxide. Yellow printing ink: shellac, povidone, titanium dioxide, D&C Yellow #10 Aluminum Lake.
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原产地英文商品名:
VICTRELIS 200mg/cap 12caps/bottle 28bottles/box
原产地英文药品名:
BOCEPREVIR
中文参考商品译名:
VICTRELIS 200毫克/胶囊 12胶囊/瓶 28瓶/盒
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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标准方案+boceprevir可改善丙型肝炎疗效
欧美学者的一项研究表明，在现行的标准治疗方案（聚乙二醇干扰素联合病毒唑）中添加丙型肝炎蛋白酶抑制剂boceprevir能够使持续应答率升高一倍。该研究2010年8月9日在线发表于《柳叶刀》（Lancet）。
聚乙二醇干扰素联合病毒唑治疗48周仅可在不足一半的1型慢性丙型肝炎病毒感染者中获得持续性病毒学应答（SVR）。研究者在美国、加拿大和欧洲的67家医疗机构520例丙型肝炎初治患者中研究了boceprevir（一种NS3丙型肝炎病毒口服蛋白酶抑制剂）联合聚乙二醇干扰素α-2b及病毒唑的疗效。
在试验的第一部分，患者被随机分配给予聚乙二醇干扰素α-2b[1.5 μg/（Kg•d）]联合病毒唑（800-1400 mg/d）治疗48周（PR48），聚乙二醇干扰素α-2b和病毒唑治疗4周继之以聚乙二醇干扰素α-2b、病毒唑和boceprevir（800 mg，每日3此）治疗24周（PR4/PRB24）或44周（PR4/PRB44），或聚乙二醇干扰素α-2b、病毒唑和boceprevir治疗28周（PRB28）或48周（PRB48）。
在试验的第二部分，275例受试者被随机分配给予PRB48或小剂量病毒唑（400-1000 mg）、聚乙二醇干扰素α-2b联合boceprevir治疗48周（低剂量PRB48）。
结果显示，使用boceprevir的4组患者SVR率均高于对照组（PRB28组为54%，P=0.013； PR4/PRB24组为56%，P=0.005；PRB48组为67%，P<0.0001；PR4/PRB44为75%，P<0.0001；PR48对照组为38%）。小剂量病毒唑与高病毒爆发率相关（27%），其复发率（22%）则与对照组（24%）相似。与对照组相比，基于boceprevir的治疗组贫血（55%对34%）和味觉障碍（27%对9%）发生率较高。
述评 意大利米兰大学米拉佐（Milazzo）博士：
丙型肝炎病毒慢性感染的标准治疗方案在疗效方面不令人满意，其相关副作用有时亦可导致治疗中止。随着对病毒生命周期和蛋白质结构的深入了解，目前已研发出以病毒复制位点为靶点的新型药物，如telaprevir和boceprevir。
上述研究结果提示，尽管未达到理想水平，但在标准治疗方案中添加NS3蛋白酶抑制剂可显著提高持续病毒学应答的出现率。需要注意的是，上述疗法也可带来附加毒性反应，而前期资料则表明boceprevir的毒性反应低于telaprevir。
此外，在出现病毒爆发的患者中，有超过1/4的标本可检出对telaprevir和boceprevir的双重耐药突变，此现象亦值得关注。
2011年5月FDA批准丙肝治疗药Boceprevir上市
默克公司日前宣布，美国食品和药品管理局（FDA）批准其慢性丙型肝炎（CHC）治疗创新新药Boceprevir（商品名Victrelis）上市。Victrelis获准与长效干扰素派罗欣（通用名聚乙二醇干扰素α）和利巴韦林联用治疗CHC基因I型慢性丙肝感染，适用于患有代偿性肝脏疾病（包括肝硬化）的18岁及以上的成年患者，这些患者以前未经治疗或之前用干扰素和利巴韦林治疗失败。
Victrelis不可用作单药治疗，只能与长效干扰素和利巴韦林联用。还没有研究Victrelis对之前用包括Victrelis或其他HCV NS3/4A蛋白酶抑制剂在内的治疗方案失败患者的疗效。
对于病历记载之前使用长效干扰素和利巴韦林联合治疗病史上无响应（截止治疗第12周，HCV-RNA下降不到2 log）的患者，Victrelis与长效干扰素和利巴韦林联用的疗效还未作研究。临床研究包括了对干扰素响应很差的患者。只用长效干扰素和利巴韦林联合治疗4周后病毒载量HCV-RNA下降不到0.5 log的患者，预计将会对用长效干扰素和利巴韦林联合治疗无响应（截止治疗第12周，HCV-RNA下降不到2 log）。
与对长效干扰素和利巴韦林联用响应较好的患者相比，干扰素响应不佳的患者接受Victrelis与长效干扰素和利巴韦林联合治疗后，出现持续病毒学应答（SVR）的可能性较低，而在治疗失败后耐药相关替代治疗的检出率却较高。
Victrelis为首个获准与长效干扰素和利巴韦林联用治疗慢性丙肝的新型丙肝病毒（HCV）蛋白酶抑制剂。长效干扰素和利巴韦林是现行慢性丙肝的标准疗法。
圣路易斯大学医学院内科教授Bruce Bacon是Victrelis的临床研究人员，他表示Victrelis是个重大进步，这是在十年内获批的首个慢性丙肝疗法。与目前的标准治疗相比，Victrelis可显著提高病人实现病毒水平不可检测的机会，从而获得SVR。对于许多患者，Victrelis可以使治疗的总持续时间缩短。
默克公司总裁兼首席执行官Kenneth C. Frazier称，该公司致力于创新而推出新药品，来满足迫切的医疗需求，Victrelis就是实现承诺的一个例子。默克公司将在一周内开始将Victrelis运达药房，因此患者很快就能买到这种新药。此外，该公司正在扩大其对慢性丙肝公众意识和教育项目的支持。 | 
