文章摘要

甲磺酸阿帕替尼在实体恶性肿瘤中的研究进展

作者: 1张 前鹏, 2成 德雷
1 和县人民医院肿瘤内科,安徽 马鞍山 238200
2 安徽省立医院介入科,中国科学技术大学第一附属医院,合肥 230001
通讯: 成 德雷 Email: 1914989044@qq.com
DOI: 10.3978/j.issn.2095-6959.2020.01.030
基金: 安徽省自然科学基金(178085QH218)。

摘要

在正常的生理条件下,新生血管的形成可以为周围组织提供能量及氧气,从而保证血流灌注。但在肿瘤患者中,血管新生出现失控,并加剧疾病进展及预后恶化。血管内皮生长因子(vascular endothelial growth factor,VEGF)及其受体(VEGFR)为诱导新生血管生成的重要调控途径。甲磺酸阿帕替尼作为国产自主研制出的抗血管生成药物,其本质为小分子的络氨酸激酶(tyrosine kinase,TK)抑制剂,其通过特异性地抑制VEGFR-2通路发挥抗血管生成作用,进而达到抗肿瘤的作用。目前国内相关指南已把其列入,特别是对于初始化疗治疗失败的晚期胃癌,其他如肺癌、乳腺癌、原发性肝细胞癌(hepatocellular carcinoma,HCC)等相关临床研究正在积极开展。
关键词: 甲磺酸阿帕替尼;抗血管生成;实体肿瘤

Research progress of mesylate apatinib in the treatment of solid malignant tumor

Authors: 1ZHANG Qianpeng, 2CHENG Delei
1 Department of Oncology, Hexian Peopl’s Hospital, Ma’anshan Anhui 238200, China
2 Department of Intervention, Anhui Provincial Hospital, First Affiliated Hospital of University of Science and Technology of China, Hefei 230001, China

CorrespondingAuthor:CHENG Delei Email: 1914989044@qq.com

Foundation: This work was supported by the Natural Science Foundation of Anhui Province, China (178085QH218).

Abstract

In physiological conditions, angiogenesis is a process responsible for the generation of new blood vessels in order to provide oxygen and nutrients to peripheral tissues and to maintain correct levels of perfusion. However, when the same process becomes uncontrolled such as in the case of cancer, the formation of new blood vessels becomes a pathological factor, which dramatically worsens patients’ clinical outcomes. The angiogenic process is majorly regulated by the interactions between tissue vascular endothelial growth factor (VEGF) and their soluble ligands (VEGFRs). Mesylate apatinib, as a domestically developed anti-angiogenesis drug, is a small-molecule tyrosine kinase (TK) inhibitor, which can exert its anti-angiogenesis effect and thereby achieve anti-tumor effect by specifically inhibiting VEGFR-2 pathway. It is now included in domestic guidelines, especially for the advanced gastric cancer. Clinical researches such as lung cancer, breast cancer, hepatocellular carcinoma (HCC) are under way.
Keywords: mesylate apatinib; anti-angiogenesis; solid tumor