Zepatier(Elbasvir/Grazoprevir Tablets)
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简体中文 |
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2016-06-30 |
| 版本号： |
1.0 |
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Win2000/WinXP/Win2003 |
| 软件类别： |
国产软件 |
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★★★★★ |
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The US Food and Drug Administration (FDA) today approved the combination drug elbasvir/grazoprevir (Zepatier, Merck) for chronic hepatitis C virus (HCV) genotypes 1 and 4 infections, another cure that does not require concomitant use of interferon with all its harsh adverse events, the agency announced.
Elbasvir/grazoprevir is indicated with or without ribavirin for adults with either genotype of HCV. Genotype 1 is the most common, while genotype 4 is one of the least common.
The new drug now will compete head to head with two other combination treatments for HCV genotype 1 that dispense with interferon — ledipasvir plus sofosbuvir (Harvoni, Gilead Sciences), and ombitasvir, paritaprevir, ritonavir, plus dasabuvir (Viekira Pak, AbbVie).
In clinical trials that established the new drug's safety and efficacy, the virus was no longer detected in the blood 12 weeks after the end of treatment in 94% to 97% of patients infected with genotype 1. This sustained virologic response (SVR) was 97% to 100% in patients with genotype 4. SVR is considered a proxy for cure rate. The participants, some of whom had cirrhosis, received elbasvir/grazoprevir once a day with or without ribavirin for 12 to 16 weeks.
Fatigue, headache, and nausea were the most common adverse events reported for patients taking the new drug without ribavirin. For those on ribavirin, the most common adverse events were anemia and headache.
The label for elbasvir/grazoprevir warns that in 1% of clinical trial participants, liver enzymes exceeded five times the upper limit of normal, generally at or after 8 weeks of treatment. Accordingly, clinicians should conduct liver-related blood tests prior to starting therapy, and afterward as well. The drug is contraindicated for patients with moderate or severe liver impairment.
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Generic Name and Formulations:
Elbasvir, grazoprevir 50mg/100mg; tabs.
Company:
Merck & Co., Inc.
Select therapeutic use: Viral infections
Indications for ZEPATIER:
Chronic HCV genotypes 1 or 4 infection with or without ribavirin (RBV).
Adult:
≥18yrs: 1 tab once daily. Genotype 1a: treatment-naive or PegIFN/RBV-experienced without baseline NS5A polymorphisms: treat for 12 weeks; with baseline NS5A polymorphisms: take with RBV for 16 weeks. Genotype 1b: treatment-naive or PegIFN/RBV-experienced: treat for 12 weeks. Genotype 1a or 1b: PegIFN/RBV/HCV NS3/4A protease inhibitor (PI)-experienced: take with RBV for 12 weeks. Genotype 4: treatment-naive: treat for 12 weeks; if PegIFN/RBV-experienced: take with RBV for 16 weeks. HCV/HIV-1 co-infected with or without cirrhosis, renal impairment including hemodialysis: follow same dosage regimen. See full labeling.
Children:
<18yrs: not established.
Contraindications:
Moderate or severe hepatic impairment. Concomitant atazanavir, carbamazepine, cyclosporine, darunavir, efavirenz, lopinavir, phenytoin, rifampin, saquinavir, St. John’s wort, tipranavir. When coadministered with ribavirin, its contraindications also apply to this combination regimen (eg, Pregnancy Cat.X).
Warnings/Precautions:
HCV genotype 1a: test for presence of virus with NS5A resistance-associated polymorphisms prior to initiation. Monitor hepatic function prior to initiation, at Week 8, and as clinically indicated; perform additional testing at Week 12 for patients receiving 16 weeks of therapy. Consider discontinuing if ALT persistently >10XULN. Discontinue if ALT elevation is accompanied with liver inflammation or increasing conjugated bilirubin, alkaline phosphatase, or INR. Pregnancy. Nursing mothers.
Interactions:
See Contraindications. Concomitant moderate CYP3A inducers or certain strong CYP3A inhibitors: not recommended. May be antagonized by nafcillin, bosentan, etravirine, modafinil. May be potentiated by ketoconazole, elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate or tenofovir alafenamide. Potentiates tacrolimus (monitor tacrolimus levels, changes in renal function), atorvastatin (limit maximum 20mg/day), rosuvastatin (limit maximum 10mg/day). May potentiate fluvastatin, lovastatin, simvastatin; use lowest effective dose of these drugs.
Pharmacological Class:
HCV NS5A inhibitor + HCV NS3/4A protease inhibitor.
Adverse Reactions:
Fatigue, headache, nausea, diarrhea, anemia.
Note:
For ribavirin specific dosing and safety information, refer to the full prescribing information.
Generic Availability:
NO
How Supplied:
Carton—2 x 14 dose packs
默沙东突破性丙肝鸡尾酒Zepatier头对头III期治疗基因型1/4丙肝疗效及安全性显著优于sofosbuvir+pegIFN/RBV方案
2016年4月21日讯 /生物谷BIOON/ --美国制药巨头默沙东（Merck & Co）近日在2016国际肝病大会上公布了丙肝鸡尾酒疗法Zepatier（elbasvir/grazoprevir，50mg/100mg）一项开放标签III期C-EDGE头对头研究的积极数据。该研究在初治及聚乙二醇干扰素/利巴韦林（pegIFN/RBV）经治基因型1和4（GT 1，GT4）丙肝患者中开展，将Zepatier与Sovaldi（sofosbuvir，索非布韦，400mg片剂）+pegIFN/RBV方案进行了头对头对比，其中Sovaldi是吉利德已上市的一款丙肝明星药。根据一项预先定义的分析数据，与sofosbuvir+pegIFN/RBV方案相比，Zepatier在疗效和安全性终点方面表现出优越性。
在全分析集(full analysis set，FAS）（n=255）中，完成治疗后12周的持续病毒学应答（SVR12，即病毒学治愈）疗效终点方面，Zepatier治疗组有99%（n=128/129）的患者实现SVR12，sofosbuvir+pegIFN/RBV方案组为90%（n=114/126）。该研究的安全性终点为预先定义的（Tier 1）安全性事件的频率，关注于耐受性、血液学副作用、肝脏相关实验室异常。
Zepatier：全球第三款突破性全口服丙肝鸡尾酒疗法
Zepatier是默沙东开发的一款突破性丙肝鸡尾酒疗法，该药是一种每日口服一次的固定剂量组合片剂，由一种HCV NS5A抑制剂elbasvir（50mg）和一种HCV NS3/4A蛋白酶抑制剂grazoprevir（100mg）组成。
在美国监管方面，Zepatier于今年1月底获FDA批准联用或不联用利巴韦林（RBV）用于基因型1和4（GT-1，GT-4）慢性丙型肝炎病毒（HCV）成人感染者的治疗。此次批准，使Zepatier成为继吉利德Harvoni和艾伯维Viekira之后获批上市的全球第3款突破性丙肝鸡尾酒疗法。
在横跨多个临床研究中，Zepatier在基因型1丙肝（GT-1 HCV）群体中的治愈率（SVR12）高达94%-97%，在基因型4丙肝（GT-4 HCV）群体中的治愈率（SVR12）高达97%-100%。SVR12（完成治疗后12周的持续病毒学应答）定义为停止治疗后第12周HCV RNA水平低于定量的下限，表明患者的丙肝感染已经治愈，即功能性治愈。
Zepatier的临床项目包括6个研究，涉及1373例基因型1和基因型4丙肝患者。数据显示，在广泛的丙肝亚群中，Zepatier均取得了很高的治愈率（SVR12），包括伴有肝硬化、伴有严重肾功能损害、伴有任何程度的HIV/HCV共感染的丙肝群体。
需要注意的是，Zepatier不适用于伴有中度至重度肝损伤（Child-Pugh B和C）的丙肝患者，同时也禁忌与以下药物联用：有机阴离子转运多肽1B1/3（OATP1B1）抑制剂（例如：阿扎那韦（atazanavir）、达芦那韦（darunavir）、洛匹那韦（ lopinavir）、沙奎那韦（saquinavir）、替拉那韦（tipranavir）、环孢素（cyclosporine））、强效细胞色素P450 3A（CYP3A）诱导剂（例如：卡马西平（carbamazepine）、苯妥英钠（phenytoin）、利福平（rifampin）、圣约翰草（St. John’s Wort）和依非韦伦（efavirenz）。如果Zepatier与利巴韦林（RBV）联用，医护人员应同时参考RBV处方信息的禁忌症、警告、注意事项、不良反应、剂量。（生物谷Bioon.com）
头对头III期C-EDGE研究的疗效数据如下：
头对头III期C-EDGE研究的安全性数据如下：
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