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特罗凯（厄洛替尼）是一种创新的生物靶向抗癌药物，适用于所有非小细胞肺癌患者，是目前世界上唯一经国际大型III期随机对照临床研究证明能够显著延长非小细胞肺癌（NSCLC）患者生命的人体表皮生长因子（EGFR）酪氨酸激酶抑制剂，每日口服一次，有希望治疗多种类型的实体肿瘤。特罗凯;显著延长生存期并有效延缓临床症状恶化。特罗凯于2004年11月获得美国FDA批准，并于2005年9月获欧盟批准上市。中国国家食品和药品监督管理局于2006年4月6日为特罗凯;颁发了进口药品许可证，用于晚期非小细胞肺癌在既往化疗失败后的三线治疗。
作用机制
与传统的化疗不同，特罗凯针对性地作用于肿瘤细胞，抑制其生长，增殖。其靶点是人体表皮生长因子受体（EGFR）。用于传递肿瘤的“生长信号”，在多种肿瘤形成及生长的过程中起着关键作用。特罗凯通过抑制表皮生长因子受体上的一种特定的酶，阻断“生长信号”，从而阻止肿瘤细胞生长。
治疗优势
特罗凯是目前世界上唯一被证明能够为肺癌患者延长生存期、提高生活质量的作用于人体表皮生长因子受体（EGFR）的靶向抗癌药物。目前大部分肺癌患者都接受化疗，通常难以耐受化疗的强烈的毒副反应。特罗凯与化疗不同的是，它靶向作用于肿瘤细胞，所以避免了典型的化疗副作用，改善了患者的生活质量。
• 研究证实特罗凯能延长患者的生命，且具有良好的安全性，还能改善生活质量，延缓肺癌症状恶化。
• 很多晚期非小细胞肺癌患者不能接受化疗。其中有很多原因，最常见的原因是患者已经太虚弱，无法承受化疗的毒副反应。
• 特罗凯是口服治疗，免去医疗机构的静脉注射费用、减轻其工作负荷，提供了额外的益处。更重要的是，特罗凯治疗能避免为处理和化疗相关的严重毒性反应而带来的巨额开销。因此，特罗凯是更为经济的治疗方法
疗效
BR.21试验是一项里程碑式的国际大型3期随机临床试验，以特罗凯与安慰剂相比较。这一试验在17个国家86个中心进行，731名经化疗失败的晚期非小细胞肺癌患者接受了治疗。
BR.21研究的主要结果：
• 特罗凯显著提高晚期非小细胞肺癌患者的生存期，中位生存期提高42.5%，一年生存率提高了45 %
• 特罗凯延缓了呕吐咳嗽、呼吸困难、疼痛等肺癌相关症状，避免了传统化疗导致的白细胞下降，恶心，等强烈的副作用，显著改善患者的生活质量
• 特罗凯可广泛应用于所有亚组（试验分析中对不同人群的分组，如性别、种族等）人群，对各种类别非小细胞肺癌患者均有效.
Tarceva benefits older lung cancer patients
New targeted lung cancer drug tarceva (erlotinib) may be especially beneficial for older lung cancer patients as per data from new research. Tarceva showed encouraging activity with relatively tolerable side effects in elderly, previously untreated patients with advanced non-small cell lung cancer as per researchers from Dana-Farber Cancer Institute in Boston. This is the first assessment of tarceva in patients who have not received any prior chemotherapy.
These phase II results are sufficiently promising to merit a Phase III trial comparing tarceva against standard chemotherapy as first line treatment of older patients with non-small cell lung cancer as per the researchers. Their findings will be presented at the 15th Annual Congress of the European Respiratory Society in Copenhagen, Denmark.
There were no complete responses to the drug, but 60 percent of the patients experienced either a partial response or had stable disease. Eight patients had partial responses, 33 had stable disease and 28 had progressive disease. The median survival was 46 weeks, and the median duration of partial response and stable disease was 65 weeks and 24 weeks, respectively.
Erlotinib tablets Tarceva™
Indication: Metastatic non-small cell lung cancer
Pharmacology: Antineoplastic; HER1/EGFR tyrosine kinase inhibitor
Usual Dose: 150 mg orally once daily, 1 hour before or 2 hours after eating
Contraindications: none known
Pregnancy Category: D
Side Effects: rash, diarrhea, nausea, vomiting, stomatitis, anorexia
fatigue
dyspnea, cough
infection
pruritus, dry skin
conjunctivitis, keratoconjunctivitis sicca
abdominal pain
abnormal liver function tests
interstitial lung disease
GI bleeding
Drug Interactions: warfarin and coumarin anticoagulants
strong CYP450 3A4 inhibitors, including:
atazanavir
clarithromycin
indinavir
itraconazole
ketoconazole
nefazodone
nelfinavir
ritonavir
saquinavir
telithromycin
troleandomycin
voriconazole
CYP450 3A4 inducers, including:
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
rifapentine
St John's wort
Warnings: Has caused serious/fatal interstitial lung disease
Monitor for pulmonary symptoms and discontinue if ILD is diagnosed
Modify dose/withhold if toxicity occurs
Monitor liver function; reduce dose or interrupt therapy if severe changes in transaminases occur
Hepatic impairment may increase exposure to erlotinib
INR elevations and bleeding have been reported
Women should avoid becoming pregnant and not breast-feed during therapy
Safety and effectiveness not established in pediatric patients
Patients should promptly report severe or persistent diarrhea, nausea, anorexia, vomiting, eye irritation, onset/exacerbation of unexplained cough or shortness of breath。
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