部份中文威罗菲尼处方资料(仅供参考) 英文名:vemurafeni 商标名:Zelboraf Tablets 中文名:威罗菲尼 生产商:罗氏(Roche) 药品简介 作用机制 是一种低分子量,口服可利用,BRAF丝氨酸-苏氨酸激酶,包括BRAFV600E的某些突变形式的抑制剂。在体外在相似浓度Vemurafenib还抑制其它激酶例如CRAF,ARAF,野生型BRAF,SRMS,ACK1,MAP4K5和FGR。在BRA基因中某些突变包括V600E导致组成性激活的BRAF蛋白,可能在缺乏生长因子中引起细胞增殖,正常需要生长因子。在有突变的BRAFV600E黑色素瘤的细胞和动物模型中Vemurafenib有抗肿瘤效应。 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。 使用限制:有野生型BRAF黑色素瘤患者中建议不使用ZELBORAF。 剂量和给药方法 (1)推荐剂量:960mg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:240mg 禁忌证 无 警告和注意事项 (1)24%患者中发生皮肤鳞状细胞癌(cuSCC)。治疗开始前和当用治疗时每2个月进行皮肤学评价。切除处理和继续治疗不调整剂量。 (2)治疗期间和再次开始治疗时曾报道严重超敏反应,包括过敏反应。经受严重超敏反应患者中终止ZELBORAF。 (3)曾报道严重皮肤学反应,包括Stevens-Johnson综合征和中毒性表皮坏死溶解。经受严重皮肤学反应患者中终止治疗。 (4)曾报道QT延长。治疗前和调整剂量后监视ECG和电解质。在第15天,治疗头3个月期间每3个月,其后每3个月,或更常如临床指示时监视ECGs。如QTc超过500 ms,短暂中断ZELBORAF,校正电解质异常,和控制对QT延长风险因子。 (5)可能发生肝实验室异常。治疗开始前和治疗期间每月,或当临床指示时监视肝酶和胆红素。 (6)曾报道光敏性。服用ZELBORAF时建议患者避免暴露阳光。 (7)曾报道严重眼科反应,包括葡萄膜炎,虹膜炎和视网膜静脉阻塞。对眼科反应常规监视患者。 (8)曾报道新原发性恶性黑色素瘤。切除处理,和继续治疗无剂量调整。如上所述,进行皮肤学监视。 (9)妊娠:可能致胎儿危害. 忠告妇女对胎儿潜在风险. (10)为了选择适于ZELBORAF治疗患者,用一种FDA-批准的检验BRAF突变。尚未在有野生型BRAF黑色素瘤患者中研究ZELBORAF的疗效和安全性。 不良反应 最常见不良反应(≥ 30%)是关节痛,皮疹,脱发,疲乏,光敏反应,恶心,瘙痒和皮肤乳头状瘤。 药物相互作用 (1)CYP底物:建议不要的同时使用ZELBORAF与被CYP3A4,CYP1A2或CYP2D6代谢治疗窗狭窄药物。如不能避免共同给药,谨慎对待和考虑减低同时CYP1A2或CYP2D6底物药物的剂量。 (2)ZELBORAF可能增加同时给药华法林[warfarin]暴露。当ZELBORAF与华法林同时使用时谨慎对待和考虑另外INR监视。 特殊人群中使用 (1)哺乳母亲:当接受ZELBORAF时终止哺乳. ZELBORAF 240MG TAB 112/EA VEMURAFENIB GENENTECH USA 50242-0090-02
Zelboraf Tablets(vemurafenib) 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. ------------------------------------------------ 产地国家:美国 原产地英文商品名: Zelboraf 240mg/tab 112tabs/bottle 原产地英文药品名: vemurafenib 中文参考商品译名: Zelboraf 240毫克/片 112片/瓶 中文参考药品译名: 威罗菲尼 生产厂家英文名: GENENTECH USA
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