甲磺酸阿帕替尼的研究现状与进展

Clinical and experimental progression of mesylate apatinib

恶性肿瘤的发生、发展与其血管生成密切相关,其中血管内皮生长因子及其受体(VEGF/VEGFR)信号通路是诱导血管新生最重要的调控途径,也是多种抗肿瘤血管生成剂的关键靶点之一。甲磺酸阿帕替尼(艾坦~)是一种新型小分子的酪氨酸激酶抑制剂,高度选择性地作用于VEGFR-2,强效抑制肿瘤血管生成,从而发挥抗肿瘤作用。阿帕替尼Ⅰ、Ⅱ、Ⅲ期注册临床试验结果表明,标准化疗失败的晚期胃癌患者应用阿帕替尼生存获益,且安全性较好。目前,阿帕替尼单药或者联合其他药物治疗肺癌、肝癌、胃癌、结直肠癌和乳腺癌等多种肿瘤的基础与临床研究正在积极开展。本文系统综述与阿帕替尼相关的基础和临床研究的现状与进展,为进一步的临床应用提供参考。

It is generally accepted that the occurrence and development of cancer are closely related to tumor angiogenesis.Vascular endothelial growth factor and its receptor（ VEGF/VEGFR） signal pathway plays an important role in regulating and controlling angiogenesis,and is also the key target of many kinds of anti-angiogenesis drugs. Mesylate apatinib is a new and small molecular antiangiogenesis drug,which can strongly against tumor angiogenesis by inhibiting VEGFR-2 with highly selectivity. A series of clinical trials confirms that there were certain objective response and obvious survival benefit to advanced gastric cancer patients treated by apatinib,who failed in the standard chemotherapy,also with better safety. Currently,trials and clinical studies of apatinib alone or in combination with other drugs for lung cancer,hepatic cancer,gastric cancer,colorectal cancer and breast cancer are carried on. This article reviewed fundamental experiments and clinical trials to provide reference for further using of apatinib in clinic.