[Research Progress of Small Molecule Anti-angiogenic Drugs in Non-small Cell Lung Cancer]

Zhongguo Fei Ai Za Zhi. 2021 Jan 20;24(1):56-62. doi: 10.3779/j.issn.1009-3419.2021.102.02.
[Article in Chinese]

Abstract

Lung cancer is one of the cancers with the highest incidence in the world, and there is no standard treatment plan after second-line progression. Tumor angiogenesis has now been identified as an important therapeutic target for malignant tumors. Small molecule multi-target vascular kinase inhibitors can inhibit tumor angiogenesis by inhibiting angiogenesis-related signal pathways. At present, a lot of clinical trials of small molecule anti-angiogenic drugs for the treatment of non-small cell lung cancer (NSCLC) have been carried out, and some vascular endothelial growth factor receptor-tyrosine kinase inhibitors (VEGFR-TKIs) have been approved for the treatment of advanced NSCLC. Based on the development status of multiple small molecule anti-angiogenic drugs at home and abroad for the treatment of NSCLC, this article summarizes the efficacy and safety studies of multiple VEGFR-TKIs and fibroblast growth factor receptor (FGFR)-TKI single agents or combination treatments [including combined with chemotherapy, epidermal growth factor receptor (EGFR)-TKIs, immunotherapy, and radiotherapy, etc.] for NSCLC, and at the same time discussed the possible existence of VEGFR-TKIs drug resistance mechanisms and efficacy predictors, etc., and prospect the future development trend and potential problems of anti-vascular treatment of NSCLC, and provide new ideas for the follow-up precision and individualized treatment of lung cancer. .

【中文题目:小分子抗血管生成药物在非小细胞肺癌中的研究进展】 【中文摘要:肺癌是世界上发病率最高的癌症之一,且尚无二线进展后的标准治疗方案,而肿瘤血管生成目前已被确定为恶性肿瘤的重要治疗靶点,小分子多靶点血管激酶抑制剂可通过抑制血管生成相关信号通路,抑制肿瘤血管的生成。目前已开展多项小分子抗血管生成药物治疗非小细胞肺癌的临床试验,且已有部分血管内皮生长因子受体酪氨酸激酶抑制剂(vascular endothelial growth factor receptor-tyrosine kinase inhibitors, VEGFR-TKIs)获批治疗晚期非小细胞肺癌,本文基于国内外多项小分子抗血管生成药物治疗非小细胞肺癌的发展现状,归纳了多个VEGFR-TKIs及成纤维细胞生长因子受体(fibroblast growth factor receptor, FGFR)-TKI单药或联合[包括分别与化疗、表皮生长因子受体(epidermal growth factor receptor, EGFR)-TKIs、免疫治疗、放疗等联合)]治疗非小细胞肺癌的疗效与安全性研究,同时探讨了VEGFR-TKIs可能存在的耐药机制及疗效预测指标等,并对未来抗血管治疗非小细胞肺癌的发展趋势以及存在的潜在问题进行展望,同时为肺癌后续的精准治疗及个体化治疗提供新的思路。 】 【中文关键词:抗血管生成抑制剂;小分子酪氨酸激酶抑制剂;肺肿瘤;进展】.

Keywords: Angiogenesis inhibitors; Lung neoplasms; Progress; Small molecular tyrosine kinase inhibitors.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / administration & dosage*
  • Animals
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / genetics
  • Carcinoma, Non-Small-Cell Lung / metabolism
  • ErbB Receptors / genetics
  • ErbB Receptors / metabolism
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / genetics
  • Lung Neoplasms / metabolism
  • Receptors, Fibroblast Growth Factor / genetics
  • Receptors, Fibroblast Growth Factor / metabolism
  • Signal Transduction / drug effects
  • Vascular Endothelial Growth Factor A / genetics
  • Vascular Endothelial Growth Factor A / metabolism

Substances

  • Angiogenesis Inhibitors
  • Receptors, Fibroblast Growth Factor
  • Vascular Endothelial Growth Factor A
  • ErbB Receptors

Grants and funding

本文受吴阶平基金资金会项目(No.320675017195)资助