血管生成被認(rèn)為是癌癥治療的潛在靶向機制,血管內(nèi)皮生長因子(VEGF)、血小板源生長因子(PDGF)、纖維母細(xì)胞生長因子(FGF)均為與血管生成相關(guān)的多能生長因子.勃林格殷格翰公司開發(fā)的新藥nintedanib,2014年10月被FDA批準(zhǔn)上市.其作為一種作用于VEGFR、PDGFR、FGFR的小分子三聯(lián)血管激酶抑制劑,用于治療特發(fā)性肺纖維化(IPF),肝衰竭和癌癥,包括轉(zhuǎn)移性非小細(xì)胞肺癌(NSCLC)、卵巢癌、前列腺癌和結(jié)腸癌、腎細(xì)胞癌等,在臨床前研究中表現(xiàn)出獨特藥理作用,在一系列臨床研究中顯示出良好的治療前景,且安全性及耐受性均較好.

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.