英文药名: Tarceva(Erlotinib Tablets) 中文药名: 特罗凯（厄洛替尼片） 品牌药生产厂家: Hoffman-La-Roche 药品名称 特罗凯（厄洛替尼盐酸盐）片剂 最初美国批准：2004 Genentech公司   最近的重大变化 警告和注意事项，国际标准化比值升高和潜在出血。   适应症 厄洛替尼是一种激酶抑制剂表明： 四个周期铂类为基础的一线化疗后维持治疗的局部晚期或转移性非小细胞肺癌（NSCLC）的疾病患者没有取得进展。 至少有一个事先化疗失败后的局部晚期或转移性非小细胞肺癌的治疗。 治疗局部晚期，不可切除或转移性胰腺癌患者的第一线，与吉西他滨的组合。   剂量和用法 非小细胞肺癌的剂量为150毫克/天。 胰腺癌的剂量是100毫克/天。 空腹至少一个小时前或2小时后，食品应采取所有剂量特罗凯。 在50毫克递减，必要时减少。   剂型和优势 片剂：25毫克，100毫克和150毫克。   禁忌 没有。   注意事项： 间质性肺疾病（ILD）样事件，包括死亡人数已很少报道。中断厄洛替尼，如果发生新的或渐进的不明原因肺部症状如呼吸困难，咳嗽，发烧，急性发作。停止厄洛替尼如果ILD的诊断。 急性肾功能衰竭（包括死亡），肾功能不全的病例被报告。在脱水的情况下中断厄洛替尼。监察脱水的危险患者的肾功能和电解质。 肝衰竭及肝肾综合征（包括死亡）的病例被报告。监测定期的肝功能测试。中断或停止厄洛替尼，如果肝功能的变化是严重的。 密切监测肝功能受损的患者。中断或停止厄洛替尼如果肝功能的变化是严重的。 据报道，包括死亡，胃肠穿孔。停止厄洛替尼。 大疱性和剥脱性皮肤疾病，包括死亡，已有报道。中断或停止厄洛替尼。 心肌梗塞/心肌缺血已被报告，包括死亡，在胰腺癌患者。 脑血管意外，包括死亡，据报道，在胰腺癌患者。 据报道，在胰腺癌患者的微血管溶血性贫血，血小板减少。 角膜穿孔和溃疡的报道。中断或停止厄洛替尼。 国际标准化比值（INR）的海拔高度和出血事件（包括死亡），与随之而来的华法林管理相关的报道。监测患者服用华法令或其他香豆素衍生物的抗凝血剂。 厄洛替尼能导致孕妇胎儿造成伤害。妇女应尽量避免怀孕时厄洛替尼。 不良反应 最常见的不良反应（> 20％）在维持治疗皮疹样的事件和腹泻。 最常见的不良反应，在第二线非小细胞肺癌（20％），皮疹，腹泻，厌食，乏力，呼吸困难，咳嗽，恶心，感染和呕吐。 胰腺癌最常见的不良反应（> 20％），乏力，皮疹，恶心，厌食，腹泻，腹痛，呕吐，体重下降，感染，水肿，发热，便秘，骨骼疼痛，呼吸困难，口腔炎和肌痛。   药物相互作用 CYP3A4抑制剂可能会增加厄洛替尼的血浆浓度。 CYP3A4诱导剂可能会降低厄洛替尼的血浆浓度。 CYP1A2的诱导剂可能会降低厄洛替尼的血浆浓度。 厄洛替尼的溶解度pH依赖性。改变上消化道pH值的药物可能会改变厄洛替尼的溶解度，因此其吸收。 吸烟降低厄洛替尼的血浆浓度。 更新日期：04/2012 提示：本品必须在有此类药物使用经验的医生指导下使用，并仅在国家肿瘤药物临床试验基地或三级甲等医院使用。 Tarceva(Erlotinib hydrochloride) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. It is marketed in the United States by Genetech and OSI Pharmaceuticals and elsewhere by Roche under the tradename Tarceva. Similar to Geftinat (gefitinib), Tarceva(Erlotinib) specifically targets theepidermal growth factor receptor (EGFR) tyrosine kinase, which is highly expressed and occasionallymutated in various forms of cancer. It binds in a reversible fashion to the adenosine triphosphate(ATP) binding site of the receptor.[1] For the signal to be transmitted, two members of the EGFR family need to come together to form a homodimer. These then use the molecule of ATP to autophosphorylate each other, which causes a conformational changein their intracellular structure, exposing a further binding site for binding proteins that cause a signal cascade to the nucleus. By inhibiting the ATP, autophosphorylation is not possible and the signal is stopped. Tarceva (Erlotinib) has shown a survival benefit in the treatment of lung cancer in phase III trials. It has been approved for the treatment of locally advanced or metastatic non-small cell lung cancer that has failed at least one prior chemotherapy regimen. In November 2005, the U.S. Food and Drug Administration (FDA) approved the use of Tarceva (Erlotinib) in combination with gemcitabine for treatment of locally advanced, unresectable, or metastaticpancreatic cancer.[2] A test for the EGFR mutation in cancer patients has been developed by Genzyme. This may predict who will respond to Tarceva(Erlotinib) and other tyrosine kinase inhibitors. It is reported that responses among patients with lung cancer are seen most often in females who were never smokers, particularly Asian women and those with adenocarcinoma cell type[citation needed]. Tarceva  (Erlotinib) has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that Tarceva(Erlotinib) may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders. The drug's US patent will expire in 2020. [4]. In India, generic pharmaceutical firm Cipla is battling with Roche against the Indian patent for this drug. In April 2009, the Delhi High Court granted a final approval to Cipla to manufacture and sell its generic version of Tarceva(Erlotinib) in India. [5] Meanwhile, another generic pharmaceutical firm - Natco is also seeking to manufacture the generic version of Tarceva(Erlotinib) in India BUT sell it to patients in Nepal using the TRIPS Agreements' Doha Declaration. Oral tablets Side effects Common side effects include: Rash occurs in the majority of patients. This resembles acne and primarily involves the face and neck. It is self-limited and resolves in the majority of cases, even with continued use. Interestingly, some clinical studies have indicated a correlation between the severity of the skin reactions and increased survival though this has not been quantitatively assessed.[8] TheJournal of Clinical Oncology reported in 2004 that "cutaneous [skin] rash seems to be a surrogate marker of clinical benefit, but this finding should be confirmed in ongoing and future studies."[9] The newsletter Lung Cancer Frontiers reported in its October 2003 issue, "Patients with moderate to severe cutaneous reactions [rashes] have a far better survival, than those with only mild reactions and much better than those with no cutaneous manifestations of drug effects. Diarrhea Loss of appetite Fatigue Rarely, interstitial pneumonitis, which is characterized by cough and increased dyspnea. This may be severe and must be considered among those patients whose breathing acutely worsens. Rarely, ingrown hairs, such as eyelashes It has also been suggested that Tarceva(Erlotinib) can cause hearing loss. Partial hair loss (by strands, not typically in clumps) Rare Side Effects: In spring, 2009, the US Food and Drug Administration issued a warning on the cancer drug Tarceva(Erlotinib). The FDA reported serious gastrointestinal tract, skin, and ocular disorders in patients taking the drug. In addition, according to a letter released by Genentech and OSI Pharmaceuticals, some people prescribed Tarceva(Erlotinib) have developed serious or fatal gastrointestinal tract perforations; "bullous, blistering, and exfoliative skin conditions, some fatal; and serious eye problems such as corneal lesions. Some of the cases, including ones which resulted in death, were suggestive ofStevens-Johnson syndrome/toxic epidermal necrolysis. Resistance to treatment A key issue with EGFR-directed treatments is that after a period of 8–12 months, the cancer cells become resistant to the treatment, most commonly by recruiting a mutated IGF-1 receptor to act as one of the EGFR partners in the homodimer, so forming a heterodimer.[12] This allows the signal to be transmitted even in the presence of an EGFR inhibitor. Some IGR-1R inhibitors are in various stages of development (based either around tyrphostins such as AG1024 or AG538[13] or pyrrolo[2,3-d]-pyrimidine derivatives such as NVP-AEW541. ------------------------------------------------------------------------ 【原产地英文商品名】:TARCEVA 25mg/tablet 30tablets/box 【原产地英文药品名】:ERLOTINIB 【中文参考商品译名】: 注：以下产品欧洲原地上市产品，不同的规格和不同价格，购买时请以电话咨询为准！ ·特罗凯 25毫克/片 30片/盒 ·特罗凯 150毫克/片 30片/盒 ·特罗凯 100毫克/片 30片/盒 【中文参考药品译名】:盐酸厄洛替尼 【曾用名】:它赛瓦,埃罗替尼(美国上市） 【生产厂家中文参考译名】:罗氏控股的美国基因泰克 【生产厂家英文名】:Roche/Genentech ------------------------------------------------------------------------------- 【原产地英文商品名】TARCEVA 150mg/tablet 30tablets/box 【原产地英文药品名】ERLOTINIB 【中文参考商品译名】 注：以下产品在美国原地上市产品，不同的规格和不同价格，购买时请以电话咨询为准！ ·特罗凯 100毫克/片 30片/盒 ·特罗凯 150毫克/片 30片/盒 ·特罗凯 25毫克/片 30片/盒 【中文参考药品译名】盐酸厄洛替尼 【曾用名】它赛瓦,埃罗替尼（土耳其上市） 【生产厂家中文参考译名】罗氏控股的美国基因泰克，美国加州南旧金山市基因泰克路1号 【生产厂家英文名】Roche/Genentech, South San Francisco, CA