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Fruquintinib: a novel antivascular endothelial growth factor receptor tyrosine kinase inhibitor for the treatment of metastatic colorectal cancer

Authors Zhang Y, Zou JY, Wang Z, Wang Y

Received 13 May 2019

Accepted for publication 28 July 2019

Published 16 August 2019 Volume 2019:11 Pages 7787—7803

DOI https://doi.org/10.2147/CMAR.S215533

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Amy Norman

Peer reviewer comments 2

Editor who approved publication: Dr Antonella D'Anneo


Ying Zhang,1 Jia-Yun Zou,1 Zhe Wang,2 Ying Wang1

1Department of Oncology, Shengjing Hospital of China Medical University, Shenyang, Liaoning Province, People’s Republic of China; 2Department of Pathology, Shengjing Hospital of China Medical University, Shenyang, Liaoning Province, People’s Republic of China

Correspondence: Ying Wang
Department of Oncology, Shengjing Hospital of China Medical University, 39 Huaxiang Street, Tiexi District, Shenyang, Liaoning Province, People’s Republic of China
Tel/fax +86 24 966 156 3311
Email wang_ying@sj-hospital.org

Abstract: Angiogenesis plays a critical role in the neoplastic growth, progression, and metastasis of colorectal cancer (CRC) in a process regulated by vascular endothelial growth factor (VEGF) family members and their receptors (VEGFR). Several small-molecule anti-VEGFR tyrosine kinase inhibitors (TKIs), such as regorafenib, famitinib, axitinib and apatinib, have been shown to be effective in treating metastatic colorectal cancer (mCRC). Fruquintinib (ELUNATE®,) is a novel oral anti-VEGFR TKI, originated and developed by Hutchison MediPharma. Fruquintinib is a potent and highly selective small-molecule inhibitor of VEGFR-1, -2 and -3. In the Phase 3 FRESCO trial, fruquintinib improved both overall survival (OS) and progression-free survival (PFS) in patients with mCRC, compared with placebo. Fruquintinib also showed an acceptable safety and tolerability profile. Based on the data from this trial, fruquintinib was approved by the China Food and Drug Administration (CFDA) in 2018, for the treatment of patients with mCRC who had undergone at least two prior standard anticancer therapies. The existing clinical trials and future prospects of fruquintinib in mCRC will be discussed in this article. In addition, to better understand the role of fruquintinib in this setting, recent advances in other anti-VEGFR TKIs for mCRC treatment are also reviewed herein.

Keywords: fruquintinib, VEGFR, tyrosine kinase inhibitor, metastatic colorectal cancer

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