Herbst Roy S
Department of Thoracic/Head and Neck Medical Oncology, The University of Texas M. D. Anderson Cancer Center, Houston, TX 77030, USA.
Clin Lung Cancer. 2006 Dec;8 Suppl 1:S23-30. doi: 10.3816/clc.2006.s.010.
The addition of antiangiogenic agents has improved overall survival in a wide variety of tumor types, including non-small-cell lung cancer (NSCLC). Antibodies to the vascular endothelial growth factor (VEGF) were the first targeted agent to yield a significant improvement in overall survival when combined with first-line chemotherapy for metastatic NSCLC. Anti-VEGF antibodies and tyrosine kinase inhibitors blocking VEGF receptor (VEGFR) activity are also being investigated in pretreated NSCLC. Initial experience with anti-VEGF antibodies suggested a mild adverse event profile. However, it has become clear with additional experience that antiangiogenic agents are associated with a distinct array of toxicities, such as hemorrhage, hypertension, thromboembolic events, and proteinuria. Furthermore, an increase in chemotherapy-associated toxicities such as neutropenia has been observed with the addition of anti-VEGF antibodies. Multitargeted small-molecule inhibitors that block activity of the VEGFR tyrosine kinase are associated with fatigue and other toxicities in addition to the aforementioned class-effect toxicities, possibly because of their inhibition of multiple signaling pathways. Currently, only patients without predominant squamous cell histology are eligible to receive bevacizumab. Trials are ongoing to address the feasibility of bevacizumab in patients who were excluded from the phase III pivotal trial. Additionally, further investigation is necessary to determine risk factors for hemorrhage with antiangiogenic agents.
抗血管生成药物的加入已改善了包括非小细胞肺癌(NSCLC)在内的多种肿瘤类型的总生存期。血管内皮生长因子(VEGF)抗体是首个与转移性NSCLC一线化疗联合使用时能显著改善总生存期的靶向药物。抗VEGF抗体和阻断VEGF受体(VEGFR)活性的酪氨酸激酶抑制剂也正在接受预处理NSCLC的研究。抗VEGF抗体的初步经验表明其不良事件较轻。然而,随着更多经验的积累,已明确抗血管生成药物与一系列独特的毒性相关,如出血、高血压、血栓栓塞事件和蛋白尿。此外,添加抗VEGF抗体后观察到化疗相关毒性如中性粒细胞减少有所增加。阻断VEGFR酪氨酸激酶活性的多靶点小分子抑制剂除了上述类效应毒性外,还与疲劳和其他毒性相关,这可能是由于它们抑制了多种信号通路。目前,只有非主要为鳞状细胞组织学类型的患者才有资格接受贝伐单抗治疗。正在进行试验以探讨贝伐单抗在被排除在III期关键试验之外的患者中的可行性。此外,还需要进一步研究以确定抗血管生成药物导致出血的危险因素。