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Target Oncol. 2015 Mar;10(1):153-70. doi: 10.1007/s11523-015-0358-9. Epub 2015 Feb 1.
Gefitinib (Iressa®) is a selective small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (EGFR TKI) indicated for the treatment of adults with locally advanced or metastatic non-small cell lung cancer (NSCLC) with activating mutations of EGFR tyrosine kinase. Large phase III or IV clinical trials in patients with locally advanced or metastatic NSCLC showed that gefitinib as first- or subsequent-line treatment significantly prolonged progression-free survival (PFS) and improved objective response rates and/or health-related quality of life parameters in patients with activating EGFR mutations and in clinically selected patients (e.g., Asian patients or never-smokers) who are more likely to harbour these mutations. Overall survival did not increase significantly with gefitinib, although post-study treatments may have had a confounding effect on this outcome. Gefitinib was generally well tolerated in these studies, with mild or moderate skin reactions, gastrointestinal disturbances and elevations in liver enzymes among the most common adverse reactions in gefitinib recipients; interstitial lung disease has also been reported in <6 % of gefitinib recipients. Compared with chemotherapy, gefitinib as first- or subsequent-line therapy provided similar or greater PFS benefit and was generally associated with fewer haematological adverse events, neurotoxicity, asthenic disorders, as well as grade ≥3 adverse events. Although the position of gefitinib with respect to other EGFR TKIs is not definitively established, current evidence indicates that gefitinib monotherapy is an effective and generally well-tolerated first- or subsequent-line treatment option for patients with NSCLC and activating EGFR mutations who have not received an EGFR TKI previously.
吉非替尼（易瑞沙）是一种选择性的小分子表皮生长因子受体（EGFR）酪氨酸激酶抑制剂（EGFR TKI），用于治疗具有 EGFR 酪氨酸激酶激活突变的局部晚期或转移性非小细胞肺癌（NSCLC）的成人患者。在局部晚期或转移性 NSCLC 患者中进行的大型 III 期或 IV 期临床试验表明，吉非替尼作为一线或二线治疗，可显著延长具有 EGFR 激活突变的患者以及在临床上选择的患者（例如亚洲患者或从不吸烟者）的无进展生存期（PFS），并提高客观缓解率和/或健康相关生活质量参数，这些患者更有可能携带这些突变。尽管在这些研究中接受吉非替尼治疗的患者总体生存率没有显著提高，但研究后的治疗可能对这一结果有影响。在这些研究中，吉非替尼通常具有良好的耐受性，最常见的不良反应包括轻度或中度皮肤反应、胃肠道紊乱和肝酶升高；间质性肺病在接受吉非替尼治疗的患者中也有报道，发生率低于 6%。与化疗相比，吉非替尼作为一线或二线治疗提供了相似或更大的 PFS 益处，并且通常与较少的血液学不良事件、神经毒性、虚弱障碍以及≥3 级不良事件相关。尽管吉非替尼相对于其他 EGFR TKI 的地位尚未确定，但现有证据表明，吉非替尼单药治疗是一种有效且通常耐受性良好的一线或二线治疗选择，适用于既往未接受过 EGFR TKI 治疗的具有 EGFR 激活突变的 NSCLC 患者。
