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血管生成在肿瘤的发生和发展中起了重要的作用.抗血管生成已成为肿瘤治疗的一个重要手段,贯穿肿瘤治疗的全过程.血管内皮生长因子受体酪氨酸激酶抑制剂(VEGFR-TKI)是小分子抗肿瘤血管生成的药物.本文介绍国内外已上市和正处于研发阶段的VEGFR-TKIs,其单药、与化疗药物联用、与靶向药物联用的治疗模式提高了晚期非小细胞肺癌(NSCLC)的客观缓解率(ORR),延长了无进展生存期(PFS),但在延长总生存期(OS)方面未见优势.并且,VEGFR-TKIs的不良反应较大.如何提高疗效,减少不良反应,将是今后研究的方向.“,”Angiogenesis plays an important role in tumor genesis and development.Therefore,anti-angiogenic therapy has become an important part in cancer therapy and throughout the entire therapy process.Vascular endothelial growth factor receptor tyrosine kinase inhibitor (VEGFR-TKI) is small molecular anti-angiogenic drug.This article introduces the domestic and international listed and researching VEGFR-TKIs.The models of single-agent/combined with chemotherapy drugs/combined with targeted drugs can improve the objective response rates (ORR)of advanced non-small cell lung cancer (NSCLC),lengthen progression-free survival(PFS).But it was failed to lengthen overall survival(OS).And the adverse effects of VEGFR-TKIs were greater.How to improve the efficacy and reduce adverse effects will be the direction of future research.