安罗替尼临床应用研究进展

Clinical research progress of anlotinib

目的血管生成对恶性肿瘤的发生、发展起着至关査要的作用。近年来,一系列抗血管生成药物在不同种类肿瘤的治疗中初见成效。安罗替尼是一种口服新型小分子多靶点酪氨酸激酶抑制剂,能有效抑制血管内皮生长因子受体(vascular endothelial growth factor receptor,VEGFR)、血小板源性生长因子受体(platelet-derived growth factor receptors,PDGFR)、成纤维细胞生长因子受体(fibroblast growth factor receptor,FGFR)、干细胞生长因子受体(c-Kit)等激酶,具有广泛的抗血管生成和抑制肿瘤生长的作用。本研究重点对其临床前研究及临床研究做系统总结。方法应用PubMed、Web of Science和全文数据库(China National Knowledge Infrastructure,CNKI)检索系统,以“安罗替尼”为关键词,检索2008-01-2018-11安罗替尼临床应用及基础研究的相关文献。共检索到中文文献16篇,英文文献20篇。纳入标准:(1)安罗替尼的大型临床研究;(2)安罗替尼相关的、严谨的临床前研究;(3)安罗替尼临床预后相关标志物研究。根据纳入标准,深入分析文献20篇。结果在多个癌种的临床试验中,安罗替尼显著延长了患者的无进展生存期和总生存期。2018-05-10,国家药品监督管理局批准安罗替尼作为晚期非小细胞肺癌(non-small cell lung cancer,NSCLC)患者的三线治疗。目前,关于安罗替尼在不同癌种中的n/m期临床实验正在开展。结论安罗替尼在肺癌等多种肿瘤的临床及临床前研究中取得令人瞩目的成果,具有广阔的临床应用前景。

OBJECTIVE Angiogenesis plays a v让al role in the occurrence and development of malignant tumors.In recent years,a series of antiangiogenic drugs have shown initial results in the treatment of different types of cancer.Anlotinib hydrochloride is a new oral small molecule multi-target tyrosine kinase inhibitor(TKI),which can effectively inhibit the kinase of VEGFR,PDGFR,FGFR,c-kit,etc.,and has a broad spectrum of inhibitory effects on tumor angiogenesis and growth.This article focuses on the systematic summary of the preclinical and clinical studies of anlotinib.METHODS PubMed,Web of Science and CNKI were used to retrieve the related literatures on Clinical research development and basic research of Anlotinib from January 2008 to January 2018.A total of 16 Chinese and 20 English literatures were retrieved.Inclusion criteria:(l)large clinical trial of Anlotinib;(2)rigorous preclinical studies related to Anlotinibj(3)biomarkers related to clinical prognosis of Anlotinib.According to the above standards,20 literatures were analyzed in depth.RESULTS In clinical trials of multiple cancers,Anlotinib significantly prolonged progression-free survival and overall survival of patients.On May 10,2018,the State Drug Administration approved Anlotinib as a third-line treatment for patients with advanced NSCLC.Currently,phaseⅡ/Ⅲclinical trials of Anlotinib in different cancers are under way.CONCLUSION Since the launch of Anlotinib,it has achieved remarkable results in clinical and preclinical studies of lung cancer and other cancers,and has broad application prospects.