Parekh Hiral, Griswold Julianne, Rini Brian
Cleveland Clinic Taussig Cancer Institute, 9500 Euclid Avenue, Mail Code R35, Cleveland, OH 44195, USA.
Future Oncol. 2016 Feb;12(3):303-11. doi: 10.2217/fon.15.322. Epub 2016 Jan 15.
Renal cell carcinoma is a cancer that results from a genetic inactivation of the VHL tumor suppressor gene leading to an upregulation of VEGF. Targeted therapies against VEGF receptors have piqued substantial interest among clinicians and researchers, and these drugs are now the standard of care in the treatment of advanced renal cell carcinoma. One of these VEGF receptor inhibitors, axitinib, has been shown to be a superior second-line therapy when compared with sorafenib. Although axitinib has clinical activity and a manageable safety profile in patients with treatment-naive metastatic renal cell carcinoma, utility in the front-line setting is area of ongoing investigation. Another area of ongoing research is dose titration of axitinib to achieve the maximum clinical benefit. Interestingly, the axitinib-related side effect of hypertension has shown to be associated with more favorable clinical outcomes. This article describes the development of axitinib and discusses the current indications for clinical use in the management of metastatic renal cell carcinoma.
肾细胞癌是一种由VHL肿瘤抑制基因的基因失活导致血管内皮生长因子（VEGF）上调而引发的癌症。针对VEGF受体的靶向治疗引起了临床医生和研究人员的极大兴趣，这些药物现已成为晚期肾细胞癌治疗的标准疗法。其中一种VEGF受体抑制剂阿昔替尼，与索拉非尼相比，已被证明是一种更优的二线治疗药物。尽管阿昔替尼在初治转移性肾细胞癌患者中具有临床活性且安全性可控，但在一线治疗中的应用仍是一个正在研究的领域。另一个正在研究的领域是阿昔替尼的剂量滴定以实现最大临床获益。有趣的是，阿昔替尼相关的高血压副作用已显示与更有利的临床结果相关。本文描述了阿昔替尼的研发过程，并讨论了其在转移性肾细胞癌管理中的当前临床应用指征。
