Zhang Tian, Park Se Eun, Hong Cierra, George Daniel J
Division of Medical Oncology, Department of Medicine, Duke Cancer Institute, Duke University Medical Center, Durham, NC 27710, USA.
Duke University School of Medicine, Durham, NC 27710, USA.
Future Oncol. 2017 Apr;13(8):755-765. doi: 10.2217/fon-2016-0358. Epub 2016 Nov 15.
Cabozantinib inhibits a variety of cellular receptors including VEGFR1-3, MET, AXL, RET, FLT3 and KIT. These signaling pathways have been shown to be important in genitourinary malignancies. Along its clinical development, it has shown most activity in advanced renal cell carcinoma; the METEOR study compared cabozantinib to everolimus and showed clinically and statistically significant improvements in both progression-free survival and overall survival. Herein, we review the development of cabozantinib in the genitourinary malignancies of renal cell carcinoma, prostate adenocarcinoma and urothelial carcinoma.
卡博替尼可抑制多种细胞受体,包括血管内皮生长因子受体1-3(VEGFR1-3)、间质-上皮转化因子(MET)、AXL受体酪氨酸激酶(AXL)、转染重排(RET)、FMS样酪氨酸激酶3(FLT3)和干细胞生长因子受体(KIT)。这些信号通路在泌尿生殖系统恶性肿瘤中已显示出重要作用。在其临床开发过程中,卡博替尼在晚期肾细胞癌中显示出最强活性;METEOR研究将卡博替尼与依维莫司进行比较,结果显示在无进展生存期和总生存期方面均有临床和统计学意义的改善。在此,我们综述卡博替尼在肾细胞癌、前列腺腺癌和尿路上皮癌等泌尿生殖系统恶性肿瘤中的研发情况。