Albiges Laurence, Gizzi Marco, Carton Edith, Escudier Bernard
Institut Gustave Roussy, 114 rue Edouard Vaillant, 94805 Villejuif, France.
Expert Rev Anticancer Ther. 2015 May;15(5):499-507. doi: 10.1586/14737140.2015.1033408.
Axitinib is the most recent targeted therapy approved by the US FDA and EMA in the treatment of metastatic renal cell carcinoma (mRCC). It is a second-generation, orally available, potent tyrosine kinase inhibitor targeting selectively VEGF receptor (VEGFR)-1, -2 and -3, resulting in inhibition of angiogenesis, metastasis and tumor growth. Based on the results of a randomized pivotal Phase III clinical trial, axitinib stands as one of the two recommended agents for patients with mRCC who progressed after first-line tyrosine kinase inhibitor therapy. Its potent and selective inhibition of VEGFR was the rationale for its development in the second-line setting after failure of prior cytokines or sunitinib. Here we examine the preclinical and clinical data of axitinib for mRCC, and its use in the treatment algorithm.
阿昔替尼是美国食品药品监督管理局(FDA)和欧洲药品管理局(EMA)最近批准用于治疗转移性肾细胞癌(mRCC)的靶向疗法。它是第二代口服有效的强效酪氨酸激酶抑制剂,选择性靶向血管内皮生长因子受体(VEGFR)-1、-2和-3,从而抑制血管生成、转移和肿瘤生长。基于一项随机关键III期临床试验的结果,阿昔替尼是一线酪氨酸激酶抑制剂治疗后病情进展的mRCC患者的两种推荐药物之一。其对VEGFR的强效和选择性抑制是其在先前细胞因子或舒尼替尼治疗失败后用于二线治疗的开发依据。在此,我们研究阿昔替尼用于mRCC的临床前和临床数据,以及其在治疗方案中的应用。