血管内皮生长因子受体和血小板源生长因子受体双靶点抑制剂的临床研究进展

Clinical development of dual tyrosine kinase inhibitors targeting vascular endothelial growth factor receptor and platelet- derived growth factor receptor

血管生成对肿瘤的生长和转移至关重要,血管内皮生长因子(VEGF)和血小板源生长因子(PDGF)是肿瘤新生血管形成中的关键性促血管生成因子,两者分别通过与其相应受体结合发挥作用,因此抑制该类因子的受体活性可有效抑制肿瘤生长。以血管内皮生长因子受体(VEGFR)和血小板源生长因子受体(PDGFR)为靶点的抗肿瘤药物的开发,在多种肿瘤治疗中取得了令人鼓舞的疗效。本文对目前进入临床研究的VEGFR和PDGFR双靶点抑制剂的研究进展进行综述。

The formation of new blood vessels is critical to the development and metastasis of neoplasm. Vascular endothelial growth factor （VEGF） and plateletderived growth factor （PDGF） are important angiogenic growth factors in the induction of angiogenesis in neoplasm, which both play a role through its receptor binding. So blocking the VEGF receptor （VEGFR） and PDGF receptor （PDGFR） can inhibit the growth of neoplasm effectively. The development of dual inhibitors that target both VEGFR and PDGFR have acquired an exciting curative effect. This paper reviewed the clinical development of dual tyrosine kinase inhibitors targeting both VEGFR and PDGFR.