Selenium substituted axitinib reduces axitinib side effects and maintains its anti-renal tumor activity

Axitinib is a potent vascular endothelial growth factor receptor (VEGFR) inhibitor, which has a strong inhibitory effect on the three isoforms of VEGFR 13. Having strong therapeutic efficacy, its broad use is limited by its side effects such as hypertension, proteinuria, cardiovascular damage, and l...

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Bibliographic Details
Published in:RSC advances 2022-08, Vol.12 (34), p.21821-21826
Main Authors: Fu, Ying, Saxu, Rengui, Ahmad Ridwan, Kadir, Zhao, Cai, Kong, Xiangshun, Rong, Yao, Zheng, Weida, Yu, Peng, Teng, Yuou
Format: Article
Language:English
Subjects:
Anticancer properties
Chemistry
Growth factors
Hypertension
Kidneys
Liver
Proteinuria
Selenium compounds
Side effects
Substitutes
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Summary:Axitinib is a potent vascular endothelial growth factor receptor (VEGFR) inhibitor, which has a strong inhibitory effect on the three isoforms of VEGFR 13. Having strong therapeutic efficacy, its broad use is limited by its side effects such as hypertension, proteinuria, cardiovascular damage, and liver and kidney dysfunction. Selenium compounds are broadly reported to have a good protective effect on cardiovascular disease, inflammation, infection, and immune function. In this study, a selenium substitute of axitinib was synthesized, and its anti-renal cell carcinoma activity and side effects were investigated. The results of the study indicated that Se-axitinib had potent antitumor activity on renal cell carcinoma (RCC), alleviated vascular hyperpermeability, and also alleviated axitinib-related side effects including hypertension, liver dysfunction and kidney dysfunction significantly. Therefore, we suggest that Se-axitinib could be a solution to the severe side effects of VEGFR inhibitors and provide evidence to improve the outcome of RCC treatment. Se-axitinib is a selenium substitution of sulfur in axitinib, which reduced the side effect of VEGFR inhibitors and maintained the potent anticancer activity of the original drug.
ISSN:2046-2069
2046-2069
DOI:10.1039/d2ra01882a