阿帕替尼抗肿瘤作用机制研究进展

Research Progress on Antitumor Mechanism of Apatinib

近年来以血管内皮生长因子(VEGF)及其受体(VEGFR)信号通路为靶点的抗血管生成药物,在恶性肿瘤的治疗中得到广泛应用。阿帕替尼是口服小分子抗血管生成药物,可特异性抑制VEGFR的酪氨酸激酶活性,进而抑制肿瘤的血管生成。2018年发布的《中国临床肿瘤学会(CSCO)胃癌诊疗指南》把阿帕替尼列为胃癌三线治疗的Ⅰ级推荐。阿帕替尼已被证实在胃癌、肺癌和乳腺癌中是有效和安全的。此外,该药物在治疗其他多种实体肿瘤中显示出巨大的潜力。本文就阿帕替尼的作用机制、临床疗效、相关疗效预测因子以及与其他抗肿瘤药物的联合用药等最新研究进展进行综述。

In recent years,antiangiogenic drugs based on VEGF and VEGFRs signaling pathway have been widely used in the treatment of malignant tumors.Apatinib is an orally bioavailable small-molecule antiangiogenic agent and can specifically inhibit the tyrosine kinase activity of VEGFR,thereby inhibiting tumor angiogenesis.Apatinib is the first-level recommendation of third-line treatment of gastric cancer in CSCO Guidelines for the Diagnosis and Treatment of Gastric Cancer published in 2018.Apatinib has been proved to be effective and safe in gastric,lung and breast cancers.In addition,the drug shows great potential in the treatment of a variety of solid tumors.This article reviews the recent progress on the mechanism,clinical efficacy,related efficacy predictors of apatinib and its combination with other antitumor drugs.