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靶向FGFR的肿瘤治疗新进展

Recent Advances in Tumor Therapy Targeting FGFR

  • 摘要: 成纤维细胞生长因子受体(FGFR)信号的异常在多种肿瘤中被发现,FGFR信号的异常参与了肿瘤发生的多项进程,包括细胞存活、增殖、炎性反应、迁移、血管生成、上皮间质转化及耐药。故FGFR是治疗肿瘤有应用前景的靶点,越来越多的FGFR抑制剂进入临床前研究及临床研究阶段,部分FGFR抑制剂已被批准应用于临床。但是获得性耐药及全身毒性等问题阻碍了FGFR抑制剂的应用。本文综述了常见FGFR抑制剂的临床应用并对其中出现的问题及解决措施作一总结。

     

    Abstract: Abnormal FGFR signaling has been found in a variety of cancers. The abnormal FGFR signaling is involved in several processes of tumorigenesis which include cell survival, proliferation, inflammation, migration, angiogenesis, epithelial-mesenchymal transformation and drug resistance. Therefore, FGFR is a very promising target for the treatment of tumors. More and more FGFR inhibitors have been developed for preclinical and clinical trials, and some FGFR inhibitors have been used in clinical applications. However, the problems such as acquired resistance and systemic toxicity have hindered the application of FGFR inhibitors. This paper reviews the clinical application of common FGFR inhibitors and summarizes the problems and solutions in their application.

     

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