Sepp-Lorenzino Laura, Thomas Kenneth A
Department of Cancer Research, Merck Research Laboratories, WP26-462, West Point, PA 19486, USA.
Expert Opin Investig Drugs. 2002 Oct;11(10):1447-65. doi: 10.1517/13543784.11.10.1447.
There is ample therapeutic opportunity for the use of antiangiogenic inhibitors in the clinic, as there are several human diseases that are dependent upon angiogenesis [1]. However, no disease has attracted as much attention as a target for antiangiogenic therapy as malignant disorders. There is a vast amount of literature acting as proof-of-principle for the use of angiogenic inhibitors as effective agents for blocking tumour-induced angiogenesis and subverting tumour growth and disease dissemination. One of the unique attractions of targeting tumour angiogenesis is that vascular endothelial cells are a genetically stable population in which acquisition of therapeutic resistance might be less efficient than in genetically unstable tumour cells [2,3]. This review covers inhibitors that target the tumour angiogenic agent vascular endothelial growth factor and its receptors as one such antiangiogenic approach. Many agents in this class are in clinical trials with limited reports of toxicity and some early evidence of clinical benefit.
在临床上，抗血管生成抑制剂有大量的治疗机会，因为有几种人类疾病依赖于血管生成[1]。然而，没有哪种疾病像恶性疾病那样，作为抗血管生成治疗的靶点受到如此多的关注。有大量文献证明，血管生成抑制剂可作为有效药物来阻断肿瘤诱导的血管生成，并颠覆肿瘤生长和疾病传播。靶向肿瘤血管生成的一个独特吸引力在于，血管内皮细胞是一个基因稳定的群体，在其中获得治疗抗性可能比在基因不稳定的肿瘤细胞中效率更低[2,3]。本综述涵盖了靶向肿瘤血管生成因子血管内皮生长因子及其受体的抑制剂，作为一种抗血管生成方法。这类中的许多药物正在进行临床试验，关于毒性的报告有限，并有一些临床获益的早期证据。
