甲磺酸阿帕替尼治疗晚期恶性肿瘤的研究进展

Research advances in mesylate apatinib in treatment of advanced malignant tumor

晚期恶性肿瘤多线治疗失败后的治疗选择是临床上所面临的难题和热点,多数恶性肿瘤的多线治疗目前没有统一标准。在恶性肿瘤的发生、发展及转移过程中,肿瘤新生血管生成起着关键作用,其中血管内皮生长因子及血管内皮生长因子受体(vascular endothelial growth factor receptor,VEGFR)的信号转导通路是诱导肿瘤血管新生最重要的调控途径,抑制此信号通路是抑制肿瘤生长和转移的一个重要研究方向。甲磺酸阿帕替尼是一种新型小分子VEGFR-2酪氨酸激酶抑制剂。研究证明,在临床前实验及临床试验中阿帕替尼对胃肠道肿瘤、非小细胞肺癌、乳腺癌等多种恶性肿瘤均表现出较高的抗肿瘤效果,且具有较高的安全性。本文就阿帕替尼治疗晚期恶性肿瘤的临床前实验和临床研究做一简单综述,为临床实践提供参考。

Treatment of advanced malignant tumors after failure of multiple lines therapy has been a hotspot of clinical research, and there is no unified standard in multiple lines of therapy so far. Neovascularization plays a key role in the tumor development and metastasis. Vascular endothelial growth factor and its receptor （VEGF/VEGFR） signal pathway are of great importance in regulating and controlling angiogenesis. Inhibition of this signal pathway is a major target in anti-tumor therapy. Mesylate apatinib is a kind of novel small molecule inhibitors of VEGFR-2 tyrosine kinase. Studies have shown that in clinical trials and preclinical experiments, apatinib shows good antitumor effect and safety in treatment of a variety of malignant tumors such as gastrointestinal cancer, non-small cell lung cancer and breast cancer. These research findings are reviewed in this paper, which may provide evidence for clinical decision.