Department of Medical Oncology, The Sixth Affiliated Hospital, Sun Yat-sen University, Guangdong Provincial Key Laboratory of Colorectal & Pelvic Floor Diseases, Guangzhou, Guangdong, PR China.
Medical Affair, Lilly Suzhou Pharmaceutical Co., Ltd, Suzhou, Jiangsu, PR China.
Future Oncol. 2019 Aug;15(22):2571-2576. doi: 10.2217/fon-2018-0454. Epub 2019 Aug 13.
Fruquintinib is a potent, highly selective and orally active inhibitor of VEGFR1, 2, 3 tyrosine kinases. It inhibits VEGF-induced VEGFR2 phosphorylation, endothelial cell proliferation and tubule formation. Currently, it has been approved for the treatment of metastatic colorectal cancer in patients who have failed at least two prior systemic antineoplastic therapies in China. However, it is not approved outside China, and there is another similar small molecular VEGFR multitarget drug approved in China, USA, Europe, etc. Here, we summarize the mechanism characteristics and clinical development of fruquintinib supporting its use in the treatment of metastastic colorectal cancer as well as explorations in other tumor types.
呋喹替尼是一种强效、高度选择性的口服血管内皮生长因子受体 1、2、3 酪氨酸激酶抑制剂。它能抑制 VEGF 诱导的 VEGFR2 磷酸化、内皮细胞增殖和管腔形成。目前，该药已在中国获批用于治疗至少接受过两种系统抗肿瘤治疗后失败的转移性结直肠癌患者。然而，该药尚未在其他国家和地区获得批准，中国还有另一种类似的小分子 VEGFR 多靶点药物获批用于美国、欧洲等国家和地区。在此，我们总结了呋喹替尼的作用机制特点和临床开发情况，以支持其用于转移性结直肠癌的治疗，并探讨了该药在其他肿瘤类型中的应用。
