Clínica Universitaria de Navarra, Pamplona, Spain.
Clin Transl Oncol. 2010 Aug;12(8):533-42. doi: 10.1007/s12094-010-0551-3.
The prognosis of metastatic colorectal cancer remains poor despite advances made in recent years, particularly with new treatments directed towards molecular targets. Cetuximab, a chimeric immunoglobulin (Ig)G1 monoclonal antibody that targets the ligand-binding domain of the epidermal growth factor receptor (EGFR), is active in metastatic colorectal cancer. As an IgG1 antibody, cetuximab may exert its antitumour efficacy through both EGFR antagonism and antibody-dependent cell-mediated cytotoxicity. The benefits of cetuximab in metastatic colorectal cancer are well documented in clinical trials and are acknowledged in the approval and licensing of this agent. There is evidence of the role of cetuximab not only in irinotecan-refractory or heavily pretreated patients, but also of the efficacy and safety of the addition of this agent to FOLFIRI (irinotecan/5-fluorouracil/leucovorin) in first-line metastatic colorectal cancer, with an enhanced effect in 5-fluorouracil patients with Kirsten rat sarcoma (KRAS) wild-type tumours. In these patients, a recent meta-analysis of the pooled Cetuximab Combined with Irinotecan in First-Line Therapy for Metastatic Colorectal Cancer (CRYSTAL) and Oxaliplatin and Cetuximab in First-Line Treatment of mCRC (OPUS) patient populations confirms that the addition of cetuximab to first-line chemotherapy achieves a statistically significant improvement in the best overall response, overall survival time, and progression-free survival (PSF) compared with chemotherapy alone. In nonresectable colorectal liver metastases, cetuximab plus FOLFOX-6 (oxaliplatin/5-fluorouracil/leucovorin) or cetuximab plus FOLFIRI increased significantly resectability of liver metastases, including R0 resections. Also, preliminary data indicate that cetuximab can be administered in a more convenient 2-week schedule in combination with standard chemotherapy. Cetuximab is generally well tolerated. Acne-form rash is the most frequent toxicity. Up to the present time, the results obtained with targeted therapy combinations are not as encouraging as initially expected. The identification of biomarkers associated with disease control, including KRAS and BRAF mutation status in patients treated with cetuximab, is changing the current management of metastatic colorectal cancer. Clinical and molecular predictive markers of response are under active evaluation in order to better select patients who could benefit from cetuximab treatment, with the aim of both optimising patient outcomes and avoiding unnecessary toxicities.
尽管近年来在转移性结直肠癌方面取得了进展,特别是针对分子靶点的新治疗方法,但转移性结直肠癌的预后仍然很差。西妥昔单抗是一种针对表皮生长因子受体(EGFR)配体结合域的嵌合免疫球蛋白(IgG1)单克隆抗体,在转移性结直肠癌中具有活性。作为一种 IgG1 抗体,西妥昔单抗可能通过 EGFR 拮抗和抗体依赖性细胞介导的细胞毒性发挥其抗肿瘤作用。西妥昔单抗在转移性结直肠癌中的疗效已在临床试验中得到充分证实,并在该药物的批准和许可中得到认可。有证据表明,西妥昔单抗不仅在伊立替康耐药或预处理过的患者中有效,而且在转移性结直肠癌一线治疗中添加该药物至 FOLFIRI(伊立替康/5-氟尿嘧啶/亚叶酸)中也具有疗效和安全性,并且在 5-氟尿嘧啶患者中具有增强作用,这些患者的 KRAS 野生型肿瘤。在这些患者中,最近对CRYSTAL(西妥昔单抗联合伊立替康一线治疗转移性结直肠癌的汇总分析)和 OPUS(奥沙利铂和西妥昔单抗一线治疗 mCRC)患者人群的荟萃分析证实,与单独化疗相比,添加西妥昔单抗至一线化疗可显著改善最佳总体反应、总生存期和无进展生存期(PSF)。在不可切除的结直肠癌肝转移中,西妥昔单抗联合 FOLFOX-6(奥沙利铂/5-氟尿嘧啶/亚叶酸)或西妥昔单抗联合 FOLFIRI 显著提高了肝转移的可切除性,包括 R0 切除。此外,初步数据表明,西妥昔单抗可以更方便地以 2 周方案与标准化疗联合使用。西妥昔单抗通常具有良好的耐受性。痤疮样皮疹是最常见的毒性。到目前为止,靶向治疗联合的结果并不像最初预期的那样令人鼓舞。识别与疾病控制相关的生物标志物,包括接受西妥昔单抗治疗的患者的 KRAS 和 BRAF 突变状态,正在改变转移性结直肠癌的当前治疗方法。正在积极评估临床和分子预测标志物的反应,以便更好地选择可能受益于西妥昔单抗治疗的患者,目的是优化患者的治疗结果并避免不必要的毒性。