美国FDA2011年8月17日批准Plexxikon Inc. HOFFMAN-LA ROCHE公司Zelboraf(vemurafenib)片治疗转移黑色素瘤。
美国食品和药品监督管理局批准Zelboraf(vemurafenib)，药物治疗后期(转移)或不可切除黑色素瘤，最危险的皮肤癌类型患者。
Zelboraf是特别适用于治疗肿瘤表达基因突变被称BRAFV600E黑色素瘤患者。在用FDA批准的诊断黑色素瘤该突变检验阴性患者中尚未研究药物。
FDA的药物评价和研究中心肿瘤药品办公室主任Richard Pazdur, M.D.说“对有后期黑色素瘤患者今年是重要一年。Zelboraf是证实改善总生存的第二个被批准新抗癌药物” “3月我们批准了Yervoy(ipilimumab)，为后期黑色素瘤另一个新治疗，接受药物后也显示延长患者生存。”
Zelboraf的评审是在FDA的优先审评计划对治疗中有重要进展或没用适当治疗的药物提供加快6个月审评药物。在药物目标日期2011年10月28日前正在批准Zelboraf和其伴随的BRAF V600E检验而伴随诊断目标日期是2011年11月12日。
在一项单个675例既往未接受治疗有BRAF V600E突变后期黑色素瘤患者国际试验确定Zelboraf'的安全性和疗效。患者被赋予接受或Zelboraf或达卡巴嗪 [dacarbazine]，另一种抗-癌治疗。试验被设计成测量总生存(患者开始治疗和死亡间时间长度)。接受Zelboraf患者未曾达到中位生存(治疗后患者生存时间长度)(77%仍生存)而接受达卡巴嗪患者中位生存为8个月(64%仍生存)。
FDA的设备和放射健康部中的在体外诊断设备评价和安全性办公室主任Alberto Gutierrez, Ph.D说：“今天批准的Zelboraf和cobas检验是发展伴随诊断和使用以保证患者以安全方式被暴露至高度有效，更个体化治疗一个大实例。”
FDA批准cobas 4800 BRAF V600突变检验是根据来自临床研究的数据也评价Zelboraf的安全性和有效性。收集患者的黑色素瘤组织样品为检验突变。
适应证和用途
ZELBORAF™是一种激酶抑制剂适用于有不可切除或转移黑色素瘤有用FDA-批准的检验检测BRAFV600E突变患者的治疗。
剂量和给药方法
   （1）推荐剂量：960 mg口服bid。
   （2）接近12小时间隔给予ZELBORAF有或无进餐。

   （3）应用一杯水完整吞服ZELBORAF。不应咀嚼或压碎ZELBORAF。

   （4）症状性不良药物反应的处理可能需要减低剂量，中断治疗，或终止ZELBORAF治疗。不建议减低剂量导致剂量低于480mg。

剂型和规格
    膜衣片：240 mg(3) 
Generic Name for ZELBORAF
Vemurafenib 240mg; tabs.

Legal Classification:
Rx

Pharmacological Class for ZELBORAF
Kinase inhibitor.

Manufacturer of ZELBORAF
Genentech, Inc.
 

Indications for ZELBORAF
Treatment of unresectable or metastatic melanoma with BRAFV600E mutation as detected by an FDA-approved test.

Adult dose for ZELBORAF
Swallow whole with water. Take in the AM and PM (approx. 12 hours apart). ≥18yrs: 960mg twice daily; until disease progression or unacceptable toxicity occurs. Dose modifications for adverse reactions or QTc prolongation: see literature. Dose reductions <480mg twice daily: not recommended.

Children's dosing for ZELBORAF
<18yrs: not recommended.

Warnings/Precautions for ZELBORAF
Not for use in wild-type BRAF melanoma. Confirm BRAFV600E mutation-positive melanoma with FDA-approved test before treating. Risk of cutaneous squamous cell carcinoma (cuSCC): ≥65 years, prior skin cancer, chronic sun exposure; if occurs, do excision and continue without dose adjustment. Do dermatologic eva luation before therapy, every 2 months during, and consider monitoring 6 months after. Long QT syndrome or QTc >500ms, uncorrectable electrolyte abnormalities, or concomitant drugs that prolong the QT interval: not recommended. Monitor electrolytes before therapy and after dose adjustments. Monitor ECG at Day 15 of treatment, monthly during the 1st 3 months, then every 3 months thereafter, or more as needed. If QTc >500ms, interrupt therapy, correct electrolytes, and control cardiac risk factors. Severe hepatic or renal impairment. Monitor liver enzymes, bilirubin before therapy and monthly, or as needed. Monitor for ophthalmologic reactions routinely. Avoid sun exposure. Pregnancy (Cat. D); avoid. Use adequate contraception during therapy and for at least 2 months after. Nursing mothers: not recommended.

Interactions for ZELBORAF
Concomitant CYP3A4, CYP1A2 or CYP2D6 substrates with narrow therapeutic indices: not recommended; if CYP1A2 or CYP2D6 substrates unavoidable, consider dose reduction of substrates. Caution with concomitant strong CYP3A4 inhibitors (eg, azole antifungals, clarithromycin) or inducers (eg, phenytoin, rifampin). May potentiate warfarin; monitor INR.

Adverse Reactions for ZELBORAF
Arthralgia, rash, alopecia, fatigue, photosensitivity, nausea, pruritus, skin papilloma; cuSCC, severe hypersensitivity or dermatologic reactions (discontinue if occurs), prolonged QTc, uveitis.

How is ZELBORAF supplied?
Tabs—120

Related Disease:
Melanoma