厄洛替尼治疗全脑放疗后复发／进展的非小细胞肺癌脑转移的疗效观察

目的对全脑放疗后复发／进展的非小细胞谛癌脑转移患者应用厄洛替尼治疗的疗效及不良反应进行观察。方法回顾性分析30例全脑放疗后复发／进展的非小细胞肺癌脑转移患者的,隘床资料。全部患者均接受厄洛替尼150mg,日1次口服,2个月后评价疗效和不良反应。结果携带EGFR外显子19／21突变者12例,状态不详者18例。全部患者颅内转移病灶的疾病控制率为56．7％,部分缓解4例（13．3％）,稳定13例（43．3％）,其中突变组部分缓解3例,稳定7例;状态不详组,部分缓解1例,稳定6例。全部患者全身病变的疾病控制率为43.3％,部分缓解3例（10％）,稳定10例（33.3％）,其中突变组部分缓解2例,稳定7例;状态不详组,部分缓解1例,稳定3例。比较两组的有效率、疾病控制率,均有统计学意义（均P〈0．05）。主要不良反应包括乏力20例（66．7％）、皮疹14倒（46．7％）、腹泻6例（20％）等,多为I度或II度。突变组较状态不详组皮疹发生率差异有统计学意义（均P〈0．05）。结论厄洛替尼对于全脑放疗后复发／进展NSCLC脑转移患者治疗有效,对EGFR基因突变者疗效更好,不良反应较轻,耐受性好。     

厄洛替尼在老年非小细胞肺癌脑转移治疗中的临床应用

目的探讨厄洛替尼(TKI)在老年非小细胞肺癌(NSCLC)脑转移治疗中的临床疗效与毒副作用。方法 32例临床确诊的老年非小细胞肺癌脑转移患者,应用厄洛替尼150 mg/d,直到病情进展。观察近期临床疗效和毒副作用。结果厄洛替尼治疗非小细胞肺癌脑转移完全缓解(CR)3例,部分缓解(PR)10例,稳定(SD)10例,进展(PD)9例,中位总生存率(OS)为10.3个月,临床缓解率90.6%,临床受益率(CR+PR+SD)71.9%,1年生存率为35.9%,2年生存率为18.6%,性别、病理类型和吸烟史与临床受益率有一定关联。厄洛替尼毒副作用主要是皮疹、腹泻、座疮、皮肤干燥等。结论上皮生长因子细胞增殖和信号传导受体(EGFR)突变、腺癌、女性、不吸烟的老年肺癌患者选用厄罗替尼临床获益较多,野生型和未检测突变的老年肺癌患者选用厄罗替尼也可部分受益,具有较好的临床疗效,毒副反应轻,可耐受。     

厄洛替尼一线治疗老年非小细胞肺癌脑转移7例疗效观察

目的探讨厄洛替尼一线治疗老年非小细胞肺癌(NSCLC)脑转移的疗效与安全性。方法对7例确诊的老年非小细胞肺癌患者,应用厄洛替尼150 mg·d-1,直到病情进展。结果厄洛替尼治疗老年非小细胞肺癌脑转移的ORR为57.1%,DCR为85.7%,中位OS为12月,1年生存率为42.9%,2年生存率为28.6%。结论厄洛替尼一线治疗老年NSCLC脑转移,具有较好的临床疗效,毒副反应轻,可耐受。     

厄洛替尼治疗晚期非小细胞肺癌的疗效观察

目的：研究厄洛替尼对晚期化疗失败的非小细胞肺癌（NSCLC）患者的疗效。方法：30例晚期NSCLC患者，口服厄洛替尼150mg·d^-1，直到病情进展或者因不良反应不能耐受为止。观察疗效，不良反应及疗效与，临床特征之间的关系。结果：31）例患者中7例部分缓解，16例稳定，7例进展，总缓解率为23．3％，疾病控制率为76．7％。Fisher’精确检验提示在肿瘤缓解率方面，年龄小于60岁者优于60岁以上患者，在肿瘤控制率方面，有皮疹患者优于无皮疹患者。结论：厄洛替尼治疗晚期化疗失败的NSCLC有一定疗效，不良反应少。     

厄洛替尼挽救治疗吉非替尼治疗失败的晚期非小细胞肺癌的疗效

目的评价厄洛替尼作为挽救方案治疗吉非替尼治疗失败的晚期非小细胞肺癌(NSCLC)的疗效及安全性。方法回顾性分析我院收治的96例采用厄洛替尼挽救治疗吉非替尼治疗后进展或复发的NSCLC患者,随访1年,观察有效率(RR)、疾病控制率(DCR)、疾病无进展生存时间(PFS)及不良反应。结果其中CR0例,PR 10例(10.42%),SD 50例(52.08%),PD 36例(37.50%),RR为10.42%,DCR为62.50%。吉非替尼治疗失败后给予化疗,进展后再给予厄洛替尼治疗者PFS为4.4个月;未间隔化疗直接给予厄洛替尼治疗者PFS为3.3个月。SD组以厄洛替尼治疗,RR、PFS分别为23.96%(23/96)、3.2个月,DCR为88.54%(85/96),非SD组DCR为52.08%(50/96),前者DCR显著高于后者(P<0.05)。结论厄洛替尼挽救治疗吉非替尼治疗失败的NSCLC具有较好的临床获益率,尤其是可提高吉非替尼治疗失败的疾病控制率,效果显著,不良反应轻微。     

康莱特注射液联合厄洛替尼治疗晚期非小细胞肺癌的观察

目的 观察康莱特注射液联合厄洛替尼治疗晚期非小细胞肺癌(NSCLC)的临床疗效和不良反应.方法 非小细胞肺癌(NSCLC)患者63例,随机分为治疗组32例和对照组31例,治疗组应用康莱特注射液联合厄洛替尼治疗,对照组采用厄洛替尼治疗,比较2组的客观疗效、生活质量及不良反应.结果 治疗组总有效率40.6%、疾病控制率75.0%,均优于对照组的32.2%和61.3%(P＜0.05);生活质量上,Karnofsky评分提高及稳定,治疗组21例占71.9%;对照组18例占58.1%,2组相比较差异有统计学意义(P＜0.05).2组的不良反应比较,皮疹、腹泻、肝功能异常及恶心呕吐差异无统计学意义(P＞0.05).结论 康莱特注射液联合厄洛替尼治疗晚期NSCLC,疗效肯定、改善患者生活质量、不良反应小.     

埃克替尼与厄洛替尼治疗晚期非小细胞肺癌的疗效对比

目的:对比分析埃克替尼与厄洛替尼治疗晚期非小细胞肺癌的临床疗效.方法:选取晚期非小细胞肺癌患者80例为研究对象,随机分为埃克替尼组与厄洛替尼组,分别采用埃克替尼与厄洛替尼进行治疗,比较两组的治疗效果.结果:埃克替尼组疾病控制率与总缓解率分别为45.0％、92.5％,厄洛替尼组分别为35.0％、87.5％,两组比较均无明显差异(P>0.05);埃克替尼组与厄洛替尼组中位肿瘤进展时间比较差异无统计学意义(P>0.05);但埃克替尼组与厄洛替尼组不良反应发生率分别为37.5％、62.5％,埃克替尼组明显低于厄洛替尼组(P<0.05).结论:采用埃克替尼与厄洛替尼对晚期非小细胞肺癌进行治疗均可取得较为理想的效果,两者疗效相似,但埃克替尼安全性高于厄洛替尼,有利于减少不良反应,可在临床上推广.     

厄洛替尼对EGFR外显子19与21突变晚期非小细胞肺癌患者的疗效比较

目的:比较厄洛替尼对表皮生长因子受体(EGFR)外显子19与21突变晚期非小细胞肺癌(NSCLC)患者的临床疗效。方法:选取我院2013年10月-2014年11月收治的EGFR突变阳性的晚期NSCLC患者,将EGFR外显子19 Del突变者分为A组,外显子21 L858R突变者分为B组,每组45例。两组患者均口服盐酸厄洛替尼片至进展。比较两组患者疾病控制率(DCR)、中位生存时间(MST)、中位进展时间(m TTP)、一年生存率以及不良反应发生率。结果:A组患者的DCR(93.02%)、一年生存率(81.40%)均明显高于B组(72.09%、60.47%)(P<0.05),MST[(15.47±2.87)个月]与m TTP[(182.00±8.24)d]均明显长于B组[(12.55±2.92)个月、(162.00±7.22)d](P<0.01),两组患者的不良反应发生率比较差异无统计学意义(P>0.05),且均未见严重不良反应发生。结论:对于晚期NSCLC患者,厄洛替尼对EGFR外显子19突变患者的疗效优于EGFR外显子21突变患者。     

吉非替尼与厄洛替尼治疗非小细胞肺癌临床疗效比较及药物经济学评价

目的比较吉非替尼与厄洛替尼治疗非小细胞肺癌的临床疗效和药物经济学评价。方法比较实验组(服用吉非替尼)38例和对照组(服用厄洛替尼)34例NSCLC患者分别给予吉非替尼和厄洛替尼治疗的临床疗效、不良反应发生情况及药物经济学评价结果。结果两组患者有效率及临床控制率比较,差异无统计学意义(P0.05);两组肿瘤进展时间及1年生存率比较,差异无统计学意义(P0.05);两组患者不良反应发生率及严重程度比较,差异无统计学意义(P0.05);实验组患者治疗费用及费用疗效比均显著低于对照组,差异具有统计学意义(P0.05)。结论吉非替尼与厄洛替尼治疗NSCLC疗效相当,但吉非替尼更加经济适用。     

化疗期间序贯应用厄洛替尼治疗晚期非小细胞肺癌的临床疗效观察

目的 观察化疗期间序贯给予厄洛替尼对晚期非小细胞肺癌(NSCLC)的疗效和不良反应.方法 58例NSCLC晚期患者化疗期间序贯给予厄洛替尼150 mg/ d,给药至疾病进展或不良反应无法耐受.采用实体瘤的疗效评价标准评价疗效.结果 58例患者中客观有效率为27.6%(16/58),疾病控制率为80.0%(47/58).主要的不良反应有皮疹、腹泻和血液系统毒性.主要的不良反应有皮疹、腹泻和血液系统毒性,皮疹多为炎性脓疱疹,常分布于颜面部、颈部、躯干和四肢等.36例出现皮疹,占62.1%.血液系统毒性主要表现为白细胞和血小板减少.结论 化疗期间序贯给予厄洛替尼治疗晚期NSCLC的近期疗效较好,不良反应耐受性好,远期疗效需进一步观察.     

Erlotinib: a new therapeutic approach for non-small cell lung cancer

Although treatment with cytotoxic agents has produced modest survival improvement in patients with stage III and IV non-small cell lung cancer (NSCLC), it appears that a plateau has been reached with currently available chemotherapeutic regimens. Increasing knowledge regarding the properties of malignant neoplasms has identified a number of potential therapeutic targets. The epidermal growth factor receptor (EGFR) is one of these targets. Preclinical models have revealed that tumour growth can be inhibited by monoclonal antibodies directed against EGFR and EGFR-specific tyrosine kinase inhibitors. Erlotinib (Tarceva?; OSI Pharmaceuticals, Genentech and Roche), a quinazoline derivative with good oral absorption, is one of several EGFR tyrosine kinases that has been studied in clinical trials. In a Phase I study, mild diarrhoea and mild rash were the most common toxicities. At a dose of 200 mg/day, diarrhoea was the dose-limiting toxicity. The observation that EGFR overexpression is relatively common in NSCLC led to a Phase II trial of erlotinib at the maximum-tolerated dose (150 mg/day) in previously treated NSCLC patients. Erlotinib produced a 12% response rate and there was no apparent relationship between response and tumour EGFR levels. More recent reports suggest that patients who develop a rash have higher responses. Based on its single agent activity, erlotinib has been evaluated in two Phase III trials which compared erlotinib plus chemotherapy to chemotherapy alone in previously untreated NSCLC patients. Erlotinib has also been compared to placebo in a Phase III trial which was limited to advanced stage NSCLC patients whose disease had progressed after two previous chemotherapy regimens. The optimum use of erlotinib in NSCLC will be determined by the results of the completed and future Phase III trials.     

Erlotinib: a new therapeutic approach for non-small cell lung cancer

Although treatment with cytotoxic agents has produced modest survival improvement in patients with stage III and IV non-small cell lung cancer (NSCLC), it appears that a plateau has been reached with currently available chemotherapeutic regimens. Increasing knowledge regarding the properties of malignant neoplasms has identified a number of potential therapeutic targets. The epidermal growth factor receptor (EGFR) is one of these targets. Preclinical models have revealed that tumour growth can be inhibited by monoclonal antibodies directed against EGFR and EGFR-specific tyrosine kinase inhibitors. Erlotinib (Tarceva trade mark; OSI Pharmaceuticals, Genentech and Roche), a quinazoline derivative with good oral absorption, is one of several EGFR tyrosine kinases that has been studied in clinical trials. In a Phase I study, mild diarrhoea and mild rash were the most common toxicities. At a dose of 200 mg/day, diarrhoea was the dose-limiting toxicity. The observation that EGFR overexpression is relatively common in NSCLC led to a Phase II trial of erlotinib at the maximum-tolerated dose (150 mg/day) in previously treated NSCLC patients. Erlotinib produced a 12% response rate and there was no apparent relationship between response and tumour EGFR levels. More recent reports suggest that patients who develop a rash have higher responses. Based on its single agent activity, erlotinib has been evaluated in two Phase III trials which compared erlotinib plus chemotherapy to chemotherapy alone in previously untreated NSCLC patients. Erlotinib has also been compared to placebo in a Phase III trial which was limited to advanced stage NSCLC patients whose disease had progressed after two previous chemotherapy regimens. The optimum use of erlotinib in NSCLC will be determined by the results of the completed and future Phase III trials.     

盐酸埃克替尼治疗EGFR突变阳性非小细胞肺癌脑转移的近期效果分析

目的 探究盐酸埃克替尼对表皮生长因子受体（EGFR）突变阳性非小细胞肺癌脑转移的近期效果。方法 选取于南阳市中心医院肿瘤医院收治的EGFR突变阳性非小细胞肺癌脑转移患者共60例,所有患者均接受盐酸埃克替尼片口服治疗,125 mg/次,3次/d。回顾性分析其近期效果。结果 患者中位无进展生存期为12.6个月（95% CI 11.85~14.42）。所有患者均接受疗效评估,其中部分缓解（PR）23例,稳定（SD）37例,EGFR突变非小细胞肺癌（NSCLC）脑转移患者的有效率（ORR）为38.33%,疾病控制率（DCR）为100%。患者的治疗史、基因突变情况、性别以及吸烟与否与治疗无进展生存期（PFS）均无显著相关性（P>0.05）;患者的治疗史,性别与是否吸烟与ORR无显著相关性（P>0.05）,而患者的基因突变情况与ORR显著相关（P<0.05）。不良反应发生情况：皮疹共出现5例,皮肤干燥9例,腹泻3例,肝功能异常2例。结论 盐酸埃克替尼治疗EGFR突变阳性非小细胞肺癌脑转移疗效显著,临床应用前景光明。     

非小细胞肺癌靶向治疗新药——厄洛替尼

厄洛替尼是一种口服、高选择性、可逆的表皮生长因子受体(EGFR)酪氨酸激酶(TK)抑制剂,它通过抑制EGFR-TK的自磷酸化反应,抑制信号转导,从而达到抑制肿瘤生长作用。一项Ⅲ期安慰剂对照临床研究结果表明,厄洛替尼每日口服150 mg单药治疗,可显著延长晚期复发性非小细胞肺癌(NSCLC)病人的生存期、延缓疾病进展和症状恶化,且耐受性较好,最常见的不良反应为皮疹和腹泻。本文对厄洛替尼的药动学和药效学特性、临床疗效和药物相互作用以及难治性晚期NSCLC病人的耐受性等作一综述。     

埃克替尼治疗30例晚期非小细胞肺癌的近期疗效及安全性分析

目的：探讨埃克替尼治疗30例NSCLC患者的近期疗效及安全性。方法：对30例患者进行随访,治疗方法为每次125mg,每日3次,口服埃克替尼药物,收集用药后2个月及4个月疗效评价及不良反应。结果：2个月疗效评价PR17例,SD7例,PD6例,客观有效率56.7%,疾病控制率80%;4个月PR15例,SD5例,PD11例,客观有效率51.7%,疾病控制率68.9%;不良反应主要是皮疹及腹泻,仅皮疹有3例Ⅲ～Ⅳ度。结论：埃克替尼治疗晚期NSCLC具有较好的近期疗效及安全性。     

厄洛替尼联合NP方案治疗非小细胞肺癌的临床疗效分析

目的：观察厄洛替尼联合NP方案治疗非小细胞肺癌的临床效果和安全性。方法将2012年3月至2012年12月在我院治疗的45例非小细胞肺癌患者随机分为两组,对照组接受NP方案治疗,治疗组接受厄洛替尼联合NP方案治疗,至少治疗2个周期后评价两组患者的临床疗效及不良反应。结果治疗组和对照组的疾病有效率（RR）分别为56.5％和45.5％,两组比较差异无统计学意义（P〉0.05）;治疗组和对照组的疾病控制率（DCR）分别为82.6％和68.2％,治疗组显著高于对照组,差异有统计学意义（P〈0.05）;治疗组和对照组的生活质量改善率分别为60.9％和40.9％,治疗组显著高于对照组,差异有统计学意义（P〈0.05）;治疗组胃肠道反应、脱发以及皮疹的发生率显著低于对照组（P〈0.05）,而两组血细胞减少、疲乏以及周围神经炎的发生率差异无统计学意义（P〉0.05）。结论厄洛替尼联合NP方案治疗非小细胞肺癌能显著提高患者的疾病控制率和生活质量,减少化疗所致的毒副反应,值得在临床推广应用。     

Erlotinib in non-small-cell lung cancer

Epidermal growth factor receptor (EGFR) plays an essential role in normal cell growth and differentiation, and is involved in tumour proliferation and survival. EGFR overexpression is a common feature in solid malignancies, including non-small-cell lung cancer (NSCLC), and is associated with poor clinical prognosis. Erlotinib is a small-molecule inhibitor of EGFR tyrosine kinase, showing a significant improvement in median survival, quality of life and related symptoms in an unselected population of advanced NSCLC patients in the second- or third-line setting. Erlotinib is well tolerated (with common toxicities including rash and diarrhoea) when administered at a standard oral daily dose of 150 mg. Further investigations are ongoing to contribute to our understanding of the role of erlotinib in NSCLC treatment.     

Erlotinib in non-small-cell lung cancer

Epidermal growth factor receptor (EGFR) plays an essential role in normal cell growth and differentiation, and is involved in tumour proliferation and survival. EGFR overexpression is a common feature in solid malignancies, including non-small-cell lung cancer (NSCLC), and is associated with poor clinical prognosis. Erlotinib is a small-molecule inhibitor of EGFR tyrosine kinase, showing a significant improvement in median survival, quality of life and related symptoms in an unselected population of advanced NSCLC patients in the second- or third-line setting. Erlotinib is well tolerated (with common toxicities including rash and diarrhoea) when administered at a standard oral daily dose of 150 mg. Further investigations are ongoing to contribute to our understanding of the role of erlotinib in NSCLC treatment.     

Reviewing the safety of erlotinib in non-small cell lung cancer

Importance of the field: Erlotinib, a potent inhibitor of EGFR activity, is approved as a monotherapy for the treatment of advanced NSCLC and in combination with gemcitabine for advanced pancreatic cancer. The oral administration and manageable toxicity of erlotinib, along with its similar efficacy to chemotherapy, make it an important option as either maintenance therapy or in second-/third-line for patients with NSCLC who have previously received first-line chemotherapy. It is also an emerging option in other treatment settings in NSCLC.

Areas covered in this review: This review summarizes safety data from major clinical trials of erlotinib in patients with advanced NSCLC, as well as post-marketing data obtained in the 5 years since this drug was first approved.

What the reader will gain: An understanding of the common toxicities expected with erlotinib in patients with advanced NSCLC.

Take home message: Erlotinib is a well-tolerated treatment option for patients with advanced NSCLC. The main adverse events of rash and diarrhea are typically mild or moderate in severity, and rarely lead to treatment withdrawal. When necessary, rash and diarrhea can be easily managed prophylactically, by active intervention or through dose reduction.