曲美替尼片Mekinist Tablets 2mg

药店国别： 产地国家：日本 处方药：是 所属类别： 2毫克/片 7片/盒 包装规格： 2毫克/片 7片/盒 计价单位：盒 生产厂家中文参考译名： 生产厂家英文名：Novartis Pharmaceuticals 原产地英文商品名：Mekinist(メキニスト錠)2MG/tabs 7tabs/box 原产地英文药品名：Trametinib Dimethyl Sulfoxide 中文参考商品译名：Mekinist(メキニスト錠)2毫克/片 7片/盒 中文参考药品译名：曲美替尼 曾用名： 简介：部份中文曲美替尼处方资料(仅供参考)药品名称：曲美替尼英文名称：trametinib分子式：C26H23FIN5O4分子量：615.39 CAS.NO： 871700-17-3规格：本品为膜包衣片剂，有0.5mg、1mg、2mg三种规格。 用法及用量： 剂量为每日1次，每次2mg，饭前1小时或饭后2小时口服。 适应症： 治疗不可切除或已经转移的BRAF V600E或V600K基因突变型黑色素瘤.产品特点及上市：曲美替尼(trametinib)是GlaxoSmithKline开发的MEK抑制剂，制剂采用DMSO溶剂合物。该药在2013年与Tafinlar同时获得FDA批准，用于治疗不可切除或已经转移的BRAF V600E或V600K基因突变型黑色素瘤，但不适用于之前已经接受BRAF抑制剂治疗的患者。在一项国际多中心、随机、开放标签、对照试验中，322例BRAF V600E或V600K阳性黑色素瘤患者按2：1分成曲美替尼治疗组和常规化疗组。结果显示，曲美替尼治疗组中位*进展生存期为4.8个月，常规化疗组中位*进展生存期为1.5个月。黑色素瘤为为*具有侵袭性的皮肤癌类型并由于皮肤疾病导致死亡。根据美国国家*研究所估计76690的美国人被诊断为黑色素瘤，2013年有9480人死于该病。 作用机理： BRAF V600E突变会激活MEK1和MEK2，Trametinib能抑制MEK1和MEK2激酶，阻止BRAF V600突变型黑色素瘤细胞的生长. 曲美替尼片英文版说明书 Use trametinib, authorised either as monotherapy or combined with dabrafenib, with caution in patients with risk factors for gastrointestinal perforationAdvice for healthcare professionals:•Use trametinib, authorised either as monotherapy or combined with dabrafenib, with caution in patients with risk factors for gastrointestinal perforation, such as gastrointestinal metastases, diverticulitis, or use of concomitant medicines that can cause gastrointestinal perforation•in these patients, be vigilant for signs and symptoms of gastrointestinal perforation. Patients should be advised to seek urgent medical attention if they develop severe abdominal pain•Suspected adverse reactions to trametinib should be reported to us on a Yellow CardTrametinib (Mekinist▼), authorised as monotherapy or combined with dabrafenib, is indicated for the treatment of adults with unresectable or metastatic melanoma with a BRAF V600 mutation.Risk of gastrointestinal perforation and colitisA review by EU medicines regulators of clinical studies and cases of suspected adverse drug reactions, reported by healthcare professionals and in the literature, has concluded that trametinib can cause gastrointestinal perforation or colitis. The review assessed all cases up to 19 November 2015 and identified 4 patients who died from gastrointestinal perforation while receiving trametinib.Case reportsOf the cases where a causal relation with trametinib (as monotherapy or combined with dabrafenib) was considered likely, most (13 of 19) were reports of gastrointestinal perforation; a few cases reported gastrointestinal perforation with colitis (3) or colitis alone (3). Most cases of gastrointestinal perforation had documented risk factors such as gastrointestinal metastases, diverticulitis, or use of concomitant medicines that can cause gastrointestinal perforation (such as non-steroidal anti-inflammatory drugs or corticosteroids).Most cases occurred in patients who received trametinib combined with dabrafenib. The risk of these adverse reactions seems to be highest within the first 2 months of starting trametinib, either as monotherapy or combined with dabrafenib.On the basis of clinical trials of trametinib (as monotherapy), the incidence of colitis or gastrointestinal perforation is approximately 1 in 200.Potential mechanismsThe inhibitory effects of trametinib on angiogenesis and gastrointestinal epithelial cell proliferation may contribute to the development of gastrointestinal perforation. In patients with gastrointestinal metastases, an additional possible mechanism is rapid tumour shrinkage due to the effects of the trametinib combined with dabrafenib which could result in intestinal perforation at the site of metastases.