Clinical research progress of fruquintinib in the treatment of malignant tumors.

IF 3 3区 医学 Q2 ONCOLOGY Investigational New Drugs Pub Date : 2024-10-01 DOI:10.1007/s10637-024-01476-6
Shihao Zhao, Wenhui Wang, Jingyi Li, Zhigang Li, Zhanbo Liu, Shunchao Zhang, Zhaoqi Chen, Hongling Wang, Xiangqi Wang, Juntao Wang
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Abstract

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.

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夫鲁喹替尼治疗恶性肿瘤的临床研究进展。
恶性肿瘤是导致全球人口死亡的一个重要原因。肿瘤血管生成被认为是恶性肿瘤的主要特征之一,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来有效抑制肿瘤生长,而且在治疗恶性肿瘤方面也取得了突破性进展。我国自主研发的抗血管生成小分子药物福罗替尼是一种强效酪氨酸激酶抑制剂,具有高选择性。它通过与血管内皮生长因子受体(VEGFR-1)、血管内皮生长因子受体(VEGFR-2)和血管内皮生长因子受体(VEGFR-3)结合并抑制它们,从而有效抑制肿瘤生长。此外,fruquintinib 还具有多种优势,包括最小的脱靶毒性、强大的耐药性特征和值得称赞的疗效。这种药物可单独使用,也可与其他疗法联合使用。它在结直肠癌、胃癌、非小细胞肺癌、乳腺癌等各种恶性肿瘤中显示出较高的有效性和生存率。因此,本文对fruquintinib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。通过综述,我们希望为fruquintinib的临床应用和后续开发提供参考。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
7.60
自引率
0.00%
发文量
121
审稿时长
1 months
期刊介绍: The development of new anticancer agents is one of the most rapidly changing aspects of cancer research. Investigational New Drugs provides a forum for the rapid dissemination of information on new anticancer agents. The papers published are of interest to the medical chemist, toxicologist, pharmacist, pharmacologist, biostatistician and clinical oncologist. Investigational New Drugs provides the fastest possible publication of new discoveries and results for the whole community of scientists developing anticancer agents.
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