Verzoni Elena, Grassi Paolo, Testa Isabella, Iacovelli Roberto, Biondani Pamela, Garanzini Enrico, De Braud Filippo, Procopio Giuseppe
Department of Medical Oncology 1, Fondazione IRCCS Istituto Nazionale Tumori, Milan, Italy.
Pharmgenomics Pers Med. 2014 Mar 27;7:107-16. doi: 10.2147/PGPM.S37098. eCollection 2014.
Antiangiogenesis options have evolved rapidly in the last few years, with an increasing number of agents currently approved by the US Food and Drug Administration and European Medicines Agency. Angiogenesis inhibitors have been shown to be very effective for the treatment of metastatic renal cancer cell. Axitinib is a third-generation inhibitor of vascular endothelial growth factor receptor and is currently being developed for the treatment of various malignancies. The pharmacokinetic properties of axitinib may have a selective therapeutic effect, with minimal adverse reactions and enhanced safety. In a large Phase III study of previously treated patients with metastatic renal cell carcinoma, axitinib achieved a longer progression-free survival than sorafenib with an acceptable safety profile and good quality of life. This review focuses on the pharmacology, pharmacokinetics, and clinical activity of axitinib in the current treatment of renal cell carcinoma. The role of axitinib in the adjuvant and/or neoadjuvant setting needs to be evaluated in further clinical trials.
在过去几年中，抗血管生成疗法发展迅速，目前有越来越多的药物获得了美国食品药品监督管理局和欧洲药品管理局的批准。血管生成抑制剂已被证明对转移性肾癌细胞的治疗非常有效。阿昔替尼是一种第三代血管内皮生长因子受体抑制剂，目前正在开发用于治疗各种恶性肿瘤。阿昔替尼的药代动力学特性可能具有选择性治疗作用，不良反应最小且安全性更高。在一项针对先前接受过治疗的转移性肾细胞癌患者的大型III期研究中，阿昔替尼比索拉非尼实现了更长的无进展生存期，且安全性可接受，生活质量良好。本综述重点关注阿昔替尼在当前肾细胞癌治疗中的药理学、药代动力学和临床活性。阿昔替尼在辅助和/或新辅助治疗中的作用需要在进一步的临床试验中进行评估。
