摘要
转移性胃癌是一类生存期很短的致死性恶性肿瘤,目前有许多针对晚期胃癌靶向治疗的研究,但结果并不理想,仅仅有少数靶向药物可以改善胃癌预后,如曲妥珠单抗和雷莫芦单抗。血管内皮生长因子(vascular endothelial growth factors,VEGF)与肿瘤发生发展密切相关,晚期胃癌患者中VEGF水平呈高表达,因此靶向VEGF被认为是胃癌治疗的新方向。在与血管生成相关的靶向药物中,阿帕替尼是一种靶向血管内皮生长因子受体2(vascular endothelial growth factors receptor,VEGFR2)的口服小分子受体酪氨酸激酶抑制剂,其口服生物利用度好并对胃癌有效。最新研究结果显示阿帕替尼作为三线方案可以改善胃癌患者生存结局,因此阿帕替尼很可能成为晚期胃癌治疗的关键药物。本文对阿帕替尼抗肿瘤机制、药代动力学、有效性及安全性、相关临床试验及最新研究进展简以综述。
Metastatic gastric cancer is a lethal disease with a very short overall survival. Although several molecular target therapies have been investigated, the results were not good. Only few agents like trastuzumab and ramucirumab could improve the prognosis of patients with metastatic gastric cancer. Vascular endothelial growth factor（VEGF） is considered to be related to the tumor development, and the expression of VEGF was high in advanced gastric cancer. Thus targeting VEGF is one of promising strategy in the treatment of gastric cancer. Among therapeutic agents which target angiogenesis, apatinib is a novel oral tyrosine kinase inhibitor targeting VEGFR2. It has a good oral bioavailability and has been confirmed to be effective in gastric cancer. The recent clinical trials displayed that as a third line treatment, apatinib could improve the outcome of gastric cancer significantly, so apatinib is very likely to be the key drug of gastric cancer. Here we review the antitumor mechanism, pharmacokinetics, efficiency, safety, relevant clinical trials and recent research progress of apatinib briefly.
出处
《临床与病理杂志》
2016年第6期815-823,共9页
Journal of Clinical and Pathological Research
基金
国家自然科学基金(81272615
81301912)~~
关键词
胃癌
阿帕替尼
临床试验
血管生成
gastric cancer
apatinib
clinical trials
angiogenesis
