Nintedanib:抗癌、抗肺纤维化的三联血管激酶抑制剂

Nintedanib: A triple angiokinase inhibitor for antitumor and anti-idiopathic pulmonary fibrosis

血管生成被认为是癌症治疗的潜在靶向机制,血管内皮生长因子(VEGF)、血小板源生长因子(PDGF)、纤维母细胞生长因子(FGF)均为与血管生成相关的多能生长因子。勃林格殷格翰公司开发的新药nintedanib,2014年10月被FDA批准上市。其作为一种作用于VEGFR、PDGFR、FGFR的小分子三联血管激酶抑制剂,用于治疗特发性肺纤维化(IPF),肝衰竭和癌症,包括转移性非小细胞肺癌(NSCLC)、卵巢癌、前列腺癌和结肠癌、肾细胞癌等,在临床前研究中表现出独特药理作用,在一系列临床研究中显示出良好的治疗前景,且安全性及耐受性均较好。

Angiogenesis is considered to be a potential targeting mechanism for cancer treatment, and vascular endothelial growth factor（VEGF）, platelet-derived growth factor（PDGF）, and fibroblast growth factor（FGF） are pluripotent growth factors associated with angiogenesis. Boehringer Ingelheim Corp developed a new drug nintedanib as a triple angiokinase inhibitor targeting at VEGF, PDGF, and FGF, which was approved by FDA in October 2014 and could be used to treat idiopathic pulmonary fibrosis（IPF）, hepatic failure, and cancers including non-small-cell lung carcinoma（NSCLC）, colon cancer, ovarian cancer, prostate cancer, renal cell carcinoma, etc. Nintedanib shows the unique pharmacokinetic and pharmacodynamic characteristics in preclinical models. And it shows a good prospect in a series of clinical studies with good safety and tolerability.