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GILOTRIF(afatinib tablets)

2014-02-28 23:20:27  作者:新特药房  来源:互联网  浏览次数:1026  文字大小:【】【】【
简介: 英文药名:GILOTRIF(afatinib tablets) 中文药名:阿法替尼片 生产厂家:德国勃林格殷格翰公司 药品介绍GILOTRIF™ (afatinib)片获批为口服使用 美国初次批准:2013 适应证和用途GILOTRIF是一 ...

英文药名:GILOTRIF(afatinib tablets)

中文药名:阿法替尼片

生产厂家:德国勃林格殷格翰公司

药品介绍
GILOTRIF™ (afatinib)片获批为口服使用

美国初次批准:2013
适应证和用途
GILOTRIF是一种激酶抑制剂适用为有转移非小细胞肺癌(NSCLC)患者一线治疗其肿瘤有当用FDA批准的测试检出的表皮生长因子受体(EGFR)外显子19缺失或外显子21(L858R)取代突变。
使用限制:尚未在肿瘤有其他EGFR突变患者中确定GILOTRIF的安全性和疗效。
剂量和给药方法
(1)推荐剂量:40mg口服,每天1次•
(2)指导患者在进餐前至少1小时或后2小时服用GILOTRIF。
剂型和规格
片:40mg,30mg,和20mg
禁忌证
无(4)
警告和注意事项
(1)腹泻:腹泻可能导致脱水和肾衰。对严重和对抗腹泻药物无反应延长腹泻不给GILOTRIF。
(2)大疱和剥脱性皮肤疾病:0.15%患者中生严重大疱,起泡,和去角质病变。对威胁生命的皮肤反应终止药物。对严重和延长皮肤反应不给GILOTRIF。
(3)间质性肺病(ILD):在1.5%患者发生。对肺症状急性发作或恶化不给GILOTRIF。如被诊断ILD终止 GILOTRIF。
(4)肝毒性:在0.18%患者中发生致命性肝损伤。用定期肝检验监视。对肝检验严重或恶化不给或终止 GILOTRIF。
(5)角膜炎:在0.8%患者中发生。不给GILOTRIF对角膜炎评价。对确证溃疡性角膜炎不给或终止GILOTRIF。
(6)胚胎胎儿毒性:可致胎儿危害。劝告女性对胎儿潜在危害和使用高效避孕。
不良反应
最常见不良反应(≥20%)是腹泻,皮疹/痤疮样皮炎,口腔炎,甲沟炎,干皮肤,食欲减低,瘙痒。)
为报告怀疑不良反应,联系Boehringer Ingelheim Pharmaceuticals,Inc.电话(800)542-6257或(800) 459-9906 TTY或FDA电话1-800-FDA-1088或www.fda.gov/medwatch.
药物相互作用
P-gp抑制剂的共同给药可能增加afatinib暴露。如不能耐受每天减低GILOTRIF 10 mg。慢性Pgp诱导剂口服的共同给药可能减低afatinib暴露。当耐受时每天增加GILOTRIF 10 mg。
在特殊人群中使用
哺乳母亲:终止药物或哺乳。
GIOTRIF:emoji: (afatinib) , Packs of 28’s tabs for all strengths – 20mg, 30mg, 40mg, 50mg – all strengths same price


FDA approves GILOTRIF™ (afatinib) as first-line treatment for metastatic non-small cell lung cancer with common EGFR mutations
Approval supported by one of the largest Phase III trials in patients with EGFR mutation-positive advanced NSCLC
Ridgefield, CT, July 12, 2013 /PRNewswire/ — Boehringer Ingelheim Pharmaceuticals, Inc. announced today that the U.S. Food and Drug Administration (FDA) has approved GILOTRIF™ (afatinib) tablets for oral use, as a new first-line (initial) treatment for patients with metastatic non-small cell lung cancer (NSCLC) with common epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test.1 Discovered and developed by Boehringer Ingelheim, GILOTRIF is the first FDA-approved oncology product from the company.
In some people, genetic mutations lead to the constant activation of the EGFR protein, which is associated with uncontrolled cell division and the development and progression of NSCLC.2 Among patients diagnosed with NSCLC (the most common form of lung cancer3), it is estimated that between 10 and 15 percent of Caucasians and approximately 40 percent of Asians have EGFR mutations4 – which in 90 percent of cases are one of the two most common EGFR mutations (Del19 or L858R).5
“The approval of GILOTRIF offers a new treatment option and provides a personalized treatment approach for patients with EGFR mutation-positive metastatic non-small cell lung cancer,” said Berthold Greifenberg, M.D., vice president, Clinical Development and Medical Affairs, Oncology. “Over the past decade, great progress has been made in understanding the biology of lung cancer and GILOTRIF is an example of how, at BI, we are translating this knowledge into a new treatment option for patients.”
To determine if a patient is eligible for GILOTRIF, physicians must conduct a test for genetic mutations – also known as biomarker testing – to determine if a common EGFR mutation is present. For this reason, and in line with FDA’s current guidance, BI collaborated with QIAGEN, a leading global provider of sample and assay technologies, on the development of a companion diagnostic for GILOTRIF. QIAGEN’s therascreen® EGFR RGQ PCR Kit was reviewed and approved by the FDA in parallel to GILOTRIF and will be used to identify patients who may be eligible for treatment.
“We are truly excited to be able to offer GILOTRIF as a new treatment option for these patients. This approval is an achievement for Boehringer Ingelheim Oncology and the many teams and individuals who committed themselves to developing this therapy based on its potential identified in the clinical trial program,” said Kevin Lokay, vice president and business unit head, Oncology, Boehringer Ingelheim Pharmaceuticals, Inc. “GILOTRIF marks the first, of what we expect will be many, oncology products to emerge from our research and development program.”
For more information about the FDA-approved therascreen® EGFR RGQ PCR Kit, please contact QIAGEN at +49 2103 29 11826.
About the LUX-Lung 3 Clinical Trial
The approval of GILOTRIF was supported in part by the LUX-Lung 3 trial – one of the largest Phase III trials conducted to date in the first-line EGFR mutation-positive, locally advanced or metastatic NSCLC treatment setting.
Results showed that within the general study population, in the GILOTRIF arm, median progression-free survival (PFS) was 11.1 months versus 6.9 months for the chemotherapy arm (pemetrexed/cisplatin) (p<0.001).1 Approximately 90 percent of patients in the study had the most common EGFR mutations (Del19 and L858R).1 In these patients, the median PFS in the GILOTRIF arm was 13.6 months versus 6.9 months in the chemotherapy arm.1
In the LUX-Lung 3 trial, the most common drug-related adverse events (AEs) observed with GILOTRIF were diarrhea (96%), rash/dermatitis acneiform (90%), stomatitis (71%), paronychia (58%), dry skin (31%), decreased appetite (29%) and pruritus (21%).1 Serious adverse events (SAEs) were reported in 29 percent of patients treated with GILOTRIF; the most frequent SAEs were diarrhea (6.6%); vomiting (4.8%); and dyspnea, fatigue, and hypokalemia (1.7% each).1
About GILOTRIF (afatinib)
GILOTRIF is indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test.1
Limitation of Use: Safety and efficacy of GILOTRIF have not been established in patients whose tumors have other EGFR mutations.1
GILOTRIF is an oral, once-daily kinase inhibitor that is designed to bind and irreversibly inhibit the following receptors: EGFR (ErbB1), HER2 (ErbB2) and ErbB4.1
IMPORTANT SAFETY INFORMATION
WARNINGS AND PRECAUTIONS
Diarrhea
•Diarrhea has resulted in dehydration with or without renal impairment; some of these cases were fatal. In the pivotal study, diarrhea occurred in 96% of patients treated with GILOTRIF (n=229), of which 15% was Grade 3 in severity and occurred within the first 6 weeks. Renal impairment as a consequence of diarrhea occurred in 6.1% of patients treated with GILOTRIF, out of which 3 (1.3%) were Grade 3.
•For patients who develop prolonged Grade 2 diarrhea lasting more than 48 hours or greater than or equal to Grade 3 diarrhea, withhold GILOTRIF until diarrhea resolves to Grade 1 or less, and resume GILOTRIF with appropriate dose reduction.
Bullous and Exfoliative Skin Disorders
•Grade 3 cutaneous reactions characterized by bullous, blistering, and exfoliating lesions occurred in 6 (0.15%) of the 3865 patients who received GILOTRIF across clinical trials. In the pivotal study, the overall incidence of cutaneous reactions consisting of rash, erythema, and acneiform rash was 90%, and the incidence of Grade 3 cutaneous reactions was 16%. In addition, the incidence of Grade 1-3 palmar-plantar erythrodysesthesia syndrome was 7%. Discontinue GILOTRIF in patients who develop life-threatening bullous, blistering, or exfoliating lesions. For patients who develop prolonged Grade 2 cutaneous adverse reactions lasting more than 7 days, intolerable Grade 2, or Grade 3 cutaneous reactions, withhold GILOTRIF until the adverse reaction resolves to Grade 1 or less, and resume GILOTRIF with appropriate dose reduction.
Interstitial Lung Disease (ILD)
•ILD or ILD-like adverse reactions (e.g., lung infiltration, pneumonitis, acute respiratory distress syndrome, or alveolitis allergic) occurred in 1.5% of the 3865 patients who received GILOTRIF across clinical trials; of these, 0.4% were fatal. The incidence of ILD appeared to be higher in patients of Asian ethnicity (2.1%) as compared to non-Asians (1.2%). In the pivotal study, the incidence of Grade ≥3 ILD was 1.3% and resulted in death in 1% of GILOTRIF-treated patients.
•Withhold GILOTRIF during evaluation of patients with suspected ILD, and discontinue GILOTRIF in patients with confirmed ILD.
Hepatic Toxicity
•In 3865 patients who received GILOTRIF across clinical trials, 10.1% had liver test abnormalities, of which 7 (0.18%) were fatal. In the pivotal study, liver test abnormalities of any grade occurred in 17.5% of the patients treated with GILOTRIF.
•Obtain periodic liver testing in patients during treatment with GILOTRIF. Withhold GILOTRIF in patients who develop worsening of liver function. In patients who develop severe hepatic impairment while taking GILOTRIF, treatment should be discontinued.
Keratitis
•Keratitis, characterized as acute or worsening eye inflammation, lacrimation, light sensitivity, blurred vision, eye pain, and/or red eye occurred in 0.8% of patients treated with GILOTRIF among 3865 patients across clinical trials. Keratitis was reported in 5 (2.2%) patients in the pivotal study, with Grade 3 in 1 (0.4%). Withhold GILOTRIF during evaluation of patients with suspected keratitis, and if diagnosis of ulcerative keratitis is confirmed, treatment with GILOTRIF should be interrupted or discontinued. If keratitis is diagnosed, the benefits and risks of continuing treatment should be carefully considered. GILOTRIF should be used with caution in patients with a history of keratitis, ulcerative keratitis, or severe dry eye. Contact lens use is also a risk factor for keratitis and ulceration.
Embryofetal Toxicity
•GILOTRIF is Pregnancy Category D. Based on its mechanism of action, GILOTRIF can cause fetal harm when administered to a pregnant woman. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
•Advise females of reproductive potential to use highly effective contraception during treatment, and for at least 2 weeks after the last dose of GILOTRIF. Advise patients to contact their healthcare provider if they become pregnant, or if pregnancy is suspected, while taking GILOTRIF.
ADVERSE REACTIONS
•The most common adverse reactions (≥20%) in the GILOTRIF-treated patients (n=229) in the pivotal study were diarrhea, rash/dermatitis acneiform, stomatitis, paronychia, dry skin, decreased appetite, pruritus.
•Serious adverse reactions were reported in 29% of patients treated with GILOTRIF. The most frequent serious adverse reactions reported in patients treated with GILOTRIF were diarrhea (6.6%); vomiting (4.8%); and dyspnea, fatigue, and hypokalemia (1.7% each). Fatal adverse reactions in GILOTRIF-treated patients included pulmonary toxicity/ILD-like adverse reactions (1.3%), sepsis (0.43%), and pneumonia (0.43%).
•More GILOTRIF-treated patients (2.2%; n=5) experienced ventricular dysfunction (defined as diastolic dysfunction, left ventricular dysfunction, or ventricular dilation; all < Grade 3) compared to chemotherapy-treated patients (0.9%; n=1).
DRUG INTERACTIONS
Effect of P-glycoprotein (P-gp) Inhibitors and Inducers
•Concomitant taking of P-gp inhibitors (including but not limited to ritonavir, cyclosporine A, ketoconazole, itraconazole, erythromycin, verapamil, quinidine, tacrolimus, nelfinavir, saquinavir, and amiodarone) with GILOTRIF can increase exposure to afatinib.
•Concomitant taking of P-gp inducers (including but not limited to rifampicin, carbamazepine, phenytoin, phenobarbital, and St. John’s wort) with GILOTRIF can decrease exposure to afatinib.
USE IN SPECIFIC POPULATIONS
Nursing Mothers
•It is not known whether afatinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from GILOTRIF, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Renal Impairment
•GILOTRIF has not been studied in patients with severely impaired renal function. Closely monitor patients with moderate (CLcr 30-59 mL/min) to severe (CLcr <30 mL/min) renal impairment and adjust GILOTRIF dose if not tolerated.
Hepatic Impairment
•GILOTRIF has not been studied in patients with severe (Child Pugh C) hepatic impairment. Closely monitor patients with severe hepatic impairment and adjust GILOTRIF dose if not tolerated.
阿法替尼(GIOTRIF)疗效和安全性再添证据
•新的疗效和安全性分析结果进一步充实了之前已经公布的、日益丰富的关于阿法替尼相较于标准化疗(培美曲塞/顺铂和吉西他滨/顺铂)的临床数据库
•最新数据证实,不可逆性ErbB家族阻滞剂阿法替尼具有可控的安全性,而且适用于EGFR突变阳性的亚洲和非亚洲肺癌患者的长期治疗[1]
•阿法替尼已经在美国、欧盟、墨西哥、智利获准应用于EGFR突变阳性的非小细胞肺癌(NSCLC)患者。在亚洲地区,阿法替尼在台湾获得了上述批准。该药在其他亚洲国家的注册申请正处于审批过程中。
•全球肺癌联盟与勃林格殷格翰公司合作启动“倾听肺癌患者的心声”旨在收集肺癌患者在真实世界中的感受
德国殷格翰2013年11月11日电 /美通社/ -- 来自两项关键性的、大规模、III期、注册临床试验(LUX-Lung 3研究和LUX-Lung 6研究)的数据显示,阿法替尼相较于化疗应用于亚洲和非亚洲患者具有优越的疗效和可控的安全性。[2,3]针对上述试验所开展的最新分析证实,阿法替尼作为一线治疗应用于EGFR突变阳性的非小细胞肺癌(NSCLC)亚洲和非亚洲患者具有一致的安全性。[1]
在NSCLC患者亚群中获得的最新数据也进一步证实了阿法替尼的疗效。基于LUX-Lung研究的其他分析也显示了阿法替尼应用于伴有不常见的EGFR突变类型[1]以及伴有转移性脑病的NSCLC患者的安全性。[5]
来自两项关键性的、大规模、III期、注册临床试验的数据显示,阿法替尼相较于化疗应用于亚洲和非亚洲患者具有优越的疗效和可控的安全性。针对上述试验所开展的最新分析证实,阿法替尼作为一线治疗应用于EGFR突变阳性的非小细胞肺癌亚洲和非亚洲患者具有一致的安全性。
在今年的世界肺癌大会(WCLC)上公布的研究结果进一步充实了日益丰富的强大的临床证据库,这些证据支持阿法替尼作为一线治疗药物应用于亚洲和非亚洲患有特定类型的晚期肺癌患者(即表皮生长因子受体(EGFR)突变阳性的NSCLC)。在中国、韩国和泰国开展的全球性临床试验 LUX-Lung 3研究及其并行试验LUX-Lung 6研究是迄今为止在EGFR突变阳性的NSCLC患者中开展过的规模最大的注册临床试验。上述试验早已证实,接受阿法替尼治疗的患者在肿瘤重新开始生长之前的生存(无进展生存,PFS)时间达到将近一年,而接受化疗的患者则略超过半年。具体而言,上述试验显示:[2,3]
•LUX-Lung 3研究:阿法替尼治疗组和培美曲塞/顺铂治疗组的PFS分别为11.1个月和6.9个月
•LUX-Lung 6研究:阿法替尼治疗组和培美曲塞/顺铂治疗组的PFS分别为11.0个月和5.6个月
(这些数据来自基于独立性回顾的主要分析。)
在LUX-Lung 6研究中,接受阿法替尼治疗组有47%患者在治疗1年后仍然存活,而且无疾病进展,化疗组则仅为2%。[3]肿瘤进展的延迟还伴有患者肺癌相关性症状(例如气促、咳嗽和胸痛)的改善以及通过肺癌标准问卷评估的生活质量的改善。[2,3]
在亚洲,肺癌占所有癌症的比例超过了14%,肺癌死亡占所有癌症死亡的比例超过了18%,尽管肺癌发生率在不同地区会有所不同。东亚地区的发病率最高,在中国大陆,每年新诊断的肺癌病例数量超过五十万,在日本和台湾地区则分别超过八万六千例和九千例。[6]由于肺癌的预后较差,从最初开始就选择最佳的治疗方案就变得非常重要。
基于LUX-Lung 3研究和LUX-Lung 6研究最新开展的安全性汇总分析证实了之前已经报告的阿法替尼应用于EGFR突变阳性的亚洲和非亚洲NSCLC患者的不良事件(AE)和耐受性特征。在上述两大患者人群中,最常见的3级副反应的发生率是相似的,包括腹泻、皮疹/痤疮和口腔炎(口腔黏膜的炎症)。[1]此外,阿法替尼的药代动力学暴露结果在上述两大患者人群中也无差异。[1]在此之前,来自LUX-Lung 3研究和LUX-Lung6研究的数据已经证实,阿法替尼的副反应是可预测、可控和可逆的,而且停药率较低。[2,3]
“最新的亚组分析证实,阿法替尼在亚洲患者中和非亚洲患者中的安全性特征是一致的,”来自位于台湾地区台北市的台湾大学医学院肿瘤研究中心主任、LUX-Lung 3研究的主要研究者 James Chih-Hsin Yang教授如此评价道。“这些数据为阿法替尼作为EGFR突变阳性的肺癌患者的有价值的治疗选择提供了进一步的支持,EGFR突变阳性的肺癌在亚洲的发生率是西方国家三倍。”
另一场独立的口头演讲则基于迄今为止规模最大的、针对伴有不常见EGFR突变类型的患者的疗效数据集,这些汇总数据来自3项前瞻性阿法替尼临床试验。这些数据显示,阿法替尼应用于伴有罕见的特定类型EGFR突变的肺癌患者的活性与该药应用于伴有常见类型的EGFR突变(缺失19, L858R)的患者的活性处于同样的范围之内。[4]
一项基于LUX-Lung 3研究的亚组分析显示,阿法替尼可作为伴有常见类型的EGFR突变和转移性脑病的肺癌患者的有效的一线治疗选择。[5]
“阿法替尼所能提供的临床受益已经通过大规模的、设计严谨的LUX-Lung临床试验计划获得了明确的体现,这些结论现在又获得了基于重要的亚组患者人群的、强有力的疗效和安全性数据的进一步支持,”勃林格殷格翰公司全球医学高级副总裁Klaus Dugi如此说道。“这些分析结果非常振奋人心,而且有望使阿法替尼成为伴有EGFR突变的亚洲和非亚洲肺癌患者的有价值的治疗选择的重要补充。”
此外,全球肺癌联盟(GLCC)还在WCLC上宣布了一项由勃林格殷格翰公司(BI)支持的创意活动,此项活动旨在进一步了解并理解肺癌患者及其家庭在现实世界中所面临的挑战。“倾听肺癌患者的心声”项目将收集来自于那些被肺癌疾病所累及的人群的反馈,包括患者及其护理者、家人、朋友、医疗专业人士和同事等。
“倾听肺癌患者的心声”项目采用独特的方法收集患者的反馈,尽可能减少基于书面文本的反馈格式,主要呈现基于视觉的调查材料。通过采用简明浏览格式的新型在线工具,受调研者只需要点击预先定义的图像、标志和基于网络的视觉材料中的元素,就能针对与之相关的议题提供反馈。这些视觉元素代表了肺癌患者及其护理人员以及家人在生活中所面临的挑战以及问题的重要性。受调研者所选取的图像或标志将透露他们最为迫切的问题和顾虑,从而反映肺癌患者随着时间推移在现实世界中的日常事项和经历。
这是有史以来首次采用上述设计方法来“倾听”肺癌患者在现实世界中的感受,并在医疗服务提供方与患者的真实处境之间搭建起沟通桥梁,从而消除间隔。调研结果将会与肺癌社区分享,从中获得的心得也将与为患者提供服务的相关人士进行分享,进而推动旨在更好地满足患者需求的新型项目、服务和宣教材料的开发。
“我们需要理解患者的感受,从而更好地为他们提供帮助,”勃林格殷格翰公司的全球医学高级副总裁Klaus Dugi教授如此说道,“患者始终处于我们在肿瘤领域所作出的承诺的核心位置,通过与GLCC的共同努力,我们就能利用‘倾听肺癌患者的心声’项目为开展全球性活动提供信息,同时有助于更加有效地支持肺癌社区,最终改善患者的生活,而且这一改善作用将不局限于治疗本身。”
“倾听肺癌患者的心声”项目的网站将于11月中旬上线,届时也将与“全球肺癌关注月”的活动相呼应。
供编辑参考信息
关于阿法替尼数据在WCLC上的公布情况
安全性亚组分析[1]
基于LUX-Lung 3研究和LUX-Lung 6研究的最新汇总性亚组分析总共纳入了468名EGFR突变阳性的患者(404名亚洲患者和64名非亚洲患者),上述患者接受阿法替尼40 mg每日一次治疗,直到发生疾病进展或发生不可耐受的不良事件为止。基于预先定义的研究标准,阿法替尼的给药剂量可增至50 mg每日一次、或降至30 mg或20 mg每日一次。所有患者报告了至少1例不良事件,最常见的不良事件包括腹泻、皮疹/痤疮和口腔炎(口腔黏膜的炎症)。导致停药的药物相关性不良事件的发生率在亚洲患者和非亚洲患者中分别为7.2%和4.7%,低于化疗组的28%。
针对不常见的突变类型的亚组分析[4]
此项分析基于被纳入LUX-Lung 2研究(II期临床试验)、LUX-Lung 3研究和LUX-Lung 6研究(两者均为III期临床试验)的EGFR突变阳性的患者。患者所伴有的突变被分为常见(Del 19 或 L858R)和不常见(所有其他单个或多个突变)两大类。通过独立性回顾对客观反应率、疾病控制、反应时间和无进展生存(PFS)进行评估。
针对转移性脑病的亚组分析[5]
在LUX-Lung 3研究中,EGFR突变阳性的患者以2:1的比例随机接受阿法替尼40 mg 每日一次治疗或最多达6个疗程的培美曲塞/顺铂标准剂量方案。伴有稳定性脑转移的患者被允许纳入。由研究者在筛选期记录脑转移。每6周进行一次肿瘤评估,直到48周为止,在此之后每12周进行一次肿瘤评估,直到出现疾病进展为止。
关于LUX-Lung 3试验[2]
LUX-Lung 3试验是规模最大的、随机、开放标记、III期注册临床试验,此项试验针对阿法替尼与由两种化疗药物培美曲塞和顺铂组成的化疗方案作为一线治疗选择应用于伴有EGFR突变的IIIb期或IV期NSCLC患者的效果进行了比较。此项试验在全球范围内纳入了345名EGFR突变阳性的NSCLC患者。LUX-Lung 3试验也是第一项在EGFR突变阳性的NSCLC患者中开展的、将培美曲塞/顺铂作为对照药物的临床试验。
在LUX-Lung 3试验中,与阿法替尼有关的最常见的3级不良事件是腹泻(14%)、皮疹(16%)和甲沟炎(11%)。与化疗(培美曲塞/顺铂)相关的最常见的3级不良事件是中性粒细胞减少症(15%)、虚弱(13%)和白细胞减少(8%)。在此项试验中,与治疗有关的不良事件有关的停药率较低(阿法替尼治疗组织和化疗组的停药率分别为8%和12%)。在阿法替尼治疗组中,有1%患者由于腹泻而停药。
关于 LUX-Lung 6试验[3]
LUX-Lung 6试验是迄今为止在伴有EGFR突变阳性的亚洲晚期肺癌患者中开展的规模最大 (n = 364)、前瞻性、注册临床试验。LUX-Lung 6试验是一项多中心、随机、开放标记的III期临床试验,对于阿法替尼相较化疗(顺铂/吉西他滨)作为一线治疗方案应用于伴有EGFR突变的晚期和转移性NSCLC的效果进行了考察。
此项试验共纳入了364名来自中国、韩国和泰国的患者(IIIB/IV期,功能状态评分 0–1,之前未接受过化疗),这些患者以2:1的比例随机接受每日口服阿法替尼* 40 mg (n=242) 或静脉接受顺铂/吉西他滨(第1天75 mg/m2/第1天和第8天1000 mg/m2,每21天一个疗程,共6个疗程,n=122)。主要终点是由中心独立审核而确定的无进展生存期。[1]
顺铂/吉西他滨是目前在中国、韩国和泰国被经常使用的NSCLC一线治疗选择。
关于阿法替尼
在欧盟、台湾地区、智利和墨西哥,阿法替尼以GIOTRIF®为商品名获准应用于肿瘤细胞具有表皮生长因子受体(EGFR)突变的转移性NSCLC的治疗。
阿法替尼在美国以GILOTRIFTM为商品名获得批准作为一线治疗药物应用于通过经FDA批准的检测方法检出存在表皮生长因子受体(EGFR)外显子19缺失或外显子21(L858R)替代突变的转移性非小细胞肺癌(NSCLC)患者。
阿法替尼是一种不可逆性ErbB家族抑制剂,该药能够不可逆性地阻断EGFR (ErbB1)以及ErbB家族的其他相关成员,上述受体在某些最为常见的肿瘤和某些死亡率较高的肿瘤的生长和播散过程中发挥了关键性的作用。阿法替尼与受体的共价、不可逆性结合与其他化合物与受体的可逆性结合的不同之处在于能够提供持久的、选择性的、完全性的ErbB家族的阻断,从而可能带来独特的治疗受益。
阿法替尼目前正处于针对NSCLC和头颈癌的III期临床试验过程中。
关于肺癌
肺癌是在全球范围内最为常见的一种癌症,每年的新发病例数达到一百六十万,其中超过半数(54%)发生在亚洲。总体而言,肺癌死亡人数占到所有亚洲癌症死亡人数18.5%。肺癌约占所有新发癌症的13%,吸烟是肺癌的主要病因。
有10%至15%的白种人NSCLC患者和 40%的亚洲NSCLC患者的肿瘤存在EGFR突变,其中约有90%的病例伴有两种EGFR突变中的一种(Del19或 L858R)。

责任编辑:admin


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