曲美替尼片Mekinist Tablets 0.5mg(Trametinib)

药店国别： 产地国家：美国 处方药：是 所属类别： 0.5毫克/片 30片/瓶 包装规格： 0.5毫克/片 30片/瓶 计价单位：瓶 生产厂家中文参考译名： 生产厂家英文名：NOVARTIS 原产地英文商品名：Mekinist 0.5mg/tab 30tabs/bottles 原产地英文药品名：trametinib 中文参考商品译名：Mekinist 0.5毫克/片 30片/瓶 中文参考药品译名：曲美替尼 曾用名： 简介：抗癌药Trametinib(商标名 Mekinist 中文译名 曲美替尼)是由诺华制药生产的新药，于2013年获美国食品药品监督管理局(FDA)批准Mekinist (曲美替尼[trametinib])与Tafinlar (达拉非尼[dabrafenib])联用治疗有不可切除的(不能用外科去除)和转移(晚期)晚期黑色素瘤患者。FDA药物评价和研究中心血液学和肿瘤产品室主任Richard Pazdur，M.D.说：“我们对一种疾病的生物途径的认识进步已允许发展第三和第四个药物Tafinlar和Mekinist，在过去两年FDA已批准为治疗转移黑色素瘤。”FDA的装置和放射性卫生中心体外诊断装置和放射学卫生室主任Alberto Gutierrez，Ph.D.说：“Tafinlar和Mekinist与对BRAF突变检测的第二个诊断伴侣共同批准证实和诊断伴侣检测和靶向癌的分子驱动物发展产品的医药承诺”。批准日期：2013年5月29日;公司: NOVARTISMEKINIST(曲美替尼[trametinib])片，为口服使用美国初始批准：2013 作用机制 Trametinib 是一种有丝分裂原-激活的胞外信号调控激酶1(MEK1)和MEK2激活以及MEK1和MEK2激酶活性的可逆性抑制。MEK蛋白胞外信号-相关激酶 (ERK)通路的上游调节物，促进细胞增殖作用。BRAF V600E突变导致BRAF通路的结构性激活其中包括MEK1和MEK2。Trametinib抑制BRAF V600突变-阳性黑色素瘤细胞在体外和体内生长。 适应证和用途 MEKINIST是一种适用于治疗有不可切除的或转移黑色素瘤当用FDA批准测试检验有BRAF V600E或V600K突变患者。使用限制：MEKINIST不适用于治疗以前曾接受BRAF抑制剂治疗患者。 剂量和给药方法 (1)开始用MEKINIST治疗前确证在肿瘤标本存在BRAF V600E或V600K突变。 (2)推荐剂量是2mg口服每天1次服用至少1小时前或进餐后至少2小时。注：(BRAF是一个人基因使一种被称为B-Raf的蛋白。基因还称为原-癌基因B-Raf和v-Raf鼠类肉瘤病毒原癌基因同源B1, 而这个蛋白更以前被称为丝氨酸/苏氨酸蛋白激酶B-Raf)剂型和规格片：0.5mg，1mg，和2mg。 禁忌证 无。 警告和注意事项 (1)心肌病：一个月治疗后再评估LVEF，和其后约每2至3个月评价。 (2)视网膜色素上皮脱落(RPED)：对任何视觉障碍进行眼科评价。如被诊断RPED不给MEKINIST和如3个月后无改善终止。 (3)视网膜静脉阻塞(RVO)：终止MEKINIST. (4)间质性肺疾病(ILD)：不给MEKINIST对新或进展性不能解释的肺症状或发现，例如咳嗽，呼吸困难，缺氧，或浸润。为治疗-相关ILD或肺炎永远终止MEKINIST。 (5)严重皮肤毒性：监视皮肤毒性和继发感染。对不能耐受2级，或3或4级皮疹尽管MEKINIST的中止在3周内未改善终止。 (6)胚胎胎儿毒性：可能致胎儿危害。忠告有生殖潜能女性对胎儿潜在风险。 不良反应 对MEKINIST最常见不良反应(≥20%)包括皮疹，腹泻，和淋巴水肿。 特殊人群中使用 (1)哺乳母亲：终止药物或哺乳。 (2)女性和男性的生殖潜能：忠告女性患者对妊娠计划和预防。可能损害生育能力。包装规格MEKINIST 0.5MG TAB 30/EA TRAMETINIB NOVARTIS 曲美替尼片英文版说明书 Two targeted cancer pills that received the FDA's nod yesterday offer physicians another set of weapons to fight the disease. They also highlight a difficulty that has plagued recent advances—the body's resistance to personalized drugs.GlaxoSmithKline's Tafinlar (dabrafenib) and Mekinist (trametinib) were sanctioned for use as single-agent oral therapies in treating unresectable or metastatic melanoma.Tafinlar got the OK to treat patients with melanoma whose tumors express the BRAF V600E gene mutation. It's in the same class as Roche/Genentech's Zelboraf, the initial BRAF inhibitor to reach market. Mekinist, the first drug in a new class called MEK inhibitors, is cleared to treat patients whose tumors express the BRAF V600E or V600K gene mutations.That gives the two new treatments a pre-defined patient population. Approximately half of melanomas arising in the skin have a BRAF gene mutation, the FDA said.The approvals add to the excitement going into the American Society of Clinical Oncology (ASCO) annual meeting, which gets under way tomorrow in Chicago. However, they also underscore a difficulty. As drug makers advance in identifying targeted therapies for particular biomarker segments, in many cases where they've developed such a treatment, the cancer comes back months later.Scientists are realizing that “targeted therapies do not lead to long-term tumor control,” said Richard Wagner, PhD, a VP at Kantar Health. “This is a problem that shadows progress.”One example is Zelboraf, the drug approved in 2011 which targets the roughly 50% of melanoma patients whose tumors carry the BRAF gene mutation. In virtually all of these patients, the tumor starts to progress again in about five months.In another case, ALK-positive patients with non-small cell lung cancer (NSCLC), tumors are held at bay for about nine months after those with the mutation take Pfizer's Xalkori (crizotinib). One of the ASCO presentations will explore data for Novartis ALK inhibitor LDK378, which appears to be the first drug able to deal with the issue of short-lived response.In a Phase I study of 123 NSCLC patients, tumors in 70% of the patients eva luated responded to the drug, and overall, tumors hadn't progressed for a median 8.6 months. That's encouraging for lung cancer patients, particularly those who relapse after crizotinib.In melanoma, it was thought that combining GSK's Mekinist with a BRAF inhibitor like Zelboraf or Tafinlar could delay progression. Tafinlar and Mekinist were approved as single agents, though, not as a combination treatment.GSK is testing the two together in a Phase III study called COMBI-AD, but it's not clear whether combined use is better than using any two melanoma drugs in sequence, Wagner said. Moreover, a statement from GSK notes that Mekinist has a specific limitation of use in patients after a BRAF inhibitor, something payers could use to deny coverage.Use of a second targeted therapy after the first could become the standard of treatment in melanoma patients whose tumors express the BRAF mutation, however, there needs to be more support from academic physicians and guideline committees before it's accepted as standard of practice, added Wagner.Meanwhile, the two GSK drugs could be left competing with Zelboraf for first-line usage. “[GSK has] succeeded in getting both drugs to market with a first-line label,” said Wagner, “but this problem of resistance of a total treatment strategy for the BRAF-mutation patients is unanswered.”Not every tumor where breakthrough treatments have been put forward develops resistance. Exceptions include the BCR-ABL inhibitors in chronic myeloid leukemia (Novartis' Gleevec and Tasigna, Bristol-Myers Squibb's Sprycel).But trying to find ways to prevent the development of resistance with targeted therapies has become another front in the war on cancer. It's also among the reasons why there is so much excitement about the immuno-oncology agents from BMS (nivolumab), Merck (MK-3475) and Roche (MPDL3280) that offer a third approach to treating the disease, beyond targeted therapies and conventional chemotherapy."We've [seen] impressive activity in multiple tumor types, long-lasting and durable results, as well as very good tolerability," said Mike King, an analyst with JMP Securities, of those agents, also known as the "programmed death," or PD-1 and PD-L1 therapies.Speaking as part of a panel assembled by Kantar Health, King said that what he thinks is compelling about the experimental agents is the "ability to get treated for a year and walk away for three to five years."Both the GSK drugs were approved with a genetic test called the THxID BRAF test, a companion diagnostic that will help determine if a patient's melanoma cells have the V600E or V600K mutation in the BRAF gene. It's sold by bioMerieux.