Zhao Shihao, Wang Wenhui, Li Jingyi, Li Zhigang, Liu Zhanbo, Zhang Shunchao, Chen Zhaoqi, Wang Hongling, Wang Xiangqi, Wang Juntao
School of Acupuncture, Moxibustion and Tuina, The Third Affiliated Hospital of Henan University of TCM, Zhengzhou, 450000, Henan, China.
Department of oncology, People's Hospital of Henan University of Chinese Medicine, Zhengzhou, 450014, Henan, China.
Invest New Drugs. 2024 Dec;42(6):612-622. doi: 10.1007/s10637-024-01476-6. Epub 2024 Oct 1.
Malignant tumors represent an important cause of mortality within the global population. Tumor angiogenesis, recognized as one of the key hallmarks of malignant tumors, is crucial for supplying essential nutrients and oxygen for tumor growth. Vascular endothelial growth factor (VEGF) and its receptor (VEGFR) are key drivers of tumor angiogenesis. Targeted therapeutic interventions not only effectively inhibit tumor growth by specifically blocking tumor angiogenesis but have also made breakthroughs in the treatment of malignant tumors. Fruquintinib, an anti-angiogenic small molecule drug developed independently in China, functions as a potent tyrosine kinase inhibitor with high selectivity. It effectively curtails tumor growth by binding to and inhibiting VEGFR-1, VEGFR-2, and VEGFR-3. Additionally, fruquintinib offers several advantages including minimal off-target toxicity, robust resistance profiles, and commendable efficacy. This agent can be used alone or in combination with other treatments. It has shown high effectiveness and survival benefits across various malignant tumors such as colorectal cancer, gastric cancer, non-small cell lung cancer, breast cancer, and other malignant tumors. Therefore, this article conducts a systematic review encompassing the mechanism of action, pharmacokinetics, clinical efficacy, and safety profile of fruquintinib. Through this review, we aimed to offer a reference for the clinical application and subsequent development of fruquintinib.
恶性肿瘤是全球人口死亡的重要原因之一。肿瘤血管生成是恶性肿瘤的关键特征之一，对于为肿瘤生长提供必需的营养物质和氧气至关重要。血管内皮生长因子（VEGF）及其受体（VEGFR）是肿瘤血管生成的关键驱动因素。靶向治疗干预不仅通过特异性阻断肿瘤血管生成有效抑制肿瘤生长，而且在恶性肿瘤治疗方面也取得了突破。呋喹替尼是中国自主研发的一种抗血管生成小分子药物，作为一种具有高选择性的强效酪氨酸激酶抑制剂发挥作用。它通过结合并抑制VEGFR-1、VEGFR-2和VEGFR-3有效抑制肿瘤生长。此外，呋喹替尼具有多种优势，包括最小的脱靶毒性、强大的耐药性和值得称赞的疗效。该药物可单独使用或与其他治疗方法联合使用。它在多种恶性肿瘤如结直肠癌、胃癌、非小细胞肺癌、乳腺癌和其他恶性肿瘤中均显示出高效性和生存获益。因此，本文对呋喹替尼的作用机制、药代动力学、临床疗效和安全性进行了系统综述。通过本综述，我们旨在为呋喹替尼的临床应用和后续开发提供参考。
