Fruquintinib: First Global Approval

Shirley, Matt

doi:10.1007/s40265-018-0998-z

Cited by 62 publications

(56 citation statements)

References 9 publications

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“…Moreover, higher ORR and DCR were observed in patients receiving fruquintinib with a manageable safety profile. Additionally, a phase I clinical trial is ongoing in the USA, exploring the efficacy and safety in non-Chinese populations [81].…”

Section: Approved Anti-angiogenic Receptor Tkismentioning

confidence: 99%

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

et al. 2019

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Angiogenesis has always been the topic of major scientific interest in the field of malignant tumors. Nowadays, targeting angiogenesis has achieved success in various carcinomas by several mechanisms, including the use of anti-angiogenic small molecule receptor tyrosine kinase inhibitors (TKIs). The development of TKIs targeting proangiogenic receptors, mainly vascular endothelial growth factor receptor (VEGFR) family, have significantly improved the outcome of certain types of cancers, like renal cell carcinoma, hepatocellular carcinoma, and colorectal carcinoma. However, the general response rate is not very satisfactory. The particular toxicity profile and resistance to anti-angiogenic targeted agents are unavoidable, and no specific marker is available to screen responsive patients to TKIs for precision therapy. To date, about 11 anti-angiogenic TKIs with different binding capacities to angiogenic receptor tyrosine kinase have been approved for the treatment of patients with advanced cancers. This review presents all approved antiangiogenic small molecule receptor TKIs so far with an emphasis on their indications and clinical efficacy. We also discuss the combination between TKIs and immune checkpoint blockade inhibitors based on the most recent exciting outcome in immunotherapy.

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Section: Approved Anti-angiogenic Receptor Tkismentioning

confidence: 99%

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

et al. 2019

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“…Cediranib is currently evaluated in a large number of clinical trials against advanced/metastatic solid tumors as single agent or in combination therapies (e.g., NSCLC, mesothelioma, glioblastoma, RCC, ovarian, prostate, breast, endometrial, colorectal, pancreatic cancers, gastrointestinal stromal tumors, and AML). Fruquintinib has been found to have weak activity against RET, FGF receptors, and KIT kinases, whereas it inhibited more efficiently VEGFRs (VEGFR-3 >> VEGFR-2 > VEGFR-1) [300]. Fruquintinib has been mostly evaluated for gastro-intestinal tumors and NSCLC and was recently approved in China for the treatment of metastatic colorectal cancer.…”

Section: Currently Approved Antiangiogenic Therapies and Experimentalmentioning

confidence: 99%

Role of VEGFs/VEGFR-1 Signaling and Its Inhibition in Modulating Tumor Invasion: Experimental Evidence in Different Metastatic Cancer Models

Ceci

Atzori

Lacal

et al. 2020

IJMS

161

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The vascular endothelial growth factor (VEGF) family members, VEGF-A, placenta growth factor (PlGF), and to a lesser extent VEGF-B, play an essential role in tumor-associated angiogenesis, tissue infiltration, and metastasis formation. Although VEGF-A can activate both VEGFR-1 and VEGFR-2 membrane receptors, PlGF and VEGF-B exclusively interact with VEGFR-1. Differently from VEGFR-2, which is involved both in physiological and pathological angiogenesis, in the adult VEGFR-1 is required only for pathological angiogenesis. Besides this role in tumor endothelium, ligand-mediated stimulation of VEGFR-1 expressed in tumor cells may directly induce cell chemotaxis and extracellular matrix invasion. Furthermore, VEGFR-1 activation in myeloid progenitors and tumor-associated macrophages favors cancer immune escape through the release of immunosuppressive cytokines. These properties have prompted a number of preclinical and clinical studies to analyze VEGFR-1 involvement in the metastatic process. The aim of the present review is to highlight the contribution of VEGFs/VEGFR-1 signaling in the progression of different tumor types and to provide an overview of the therapeutic approaches targeting VEGFR-1 currently under investigation.

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“…Fruquintinib (ELUNATE ® ) was originated and developed by Hutchison MediPharma and then co-developed and commercialized by Eli Lilly and Company in October 2013 under a licensing agreement in China 20. On September 4, 2018, fruquintinib was granted approval by CFDA to treat patients with mCRC who had failed at least two prior standard antitumor therapies, including fluoropyrimidine, oxaliplatin and irinotecan, with or without prior use of anti-VEGF or anti-epidermal growth factor receptor (EGFR) treatment 21.…”

Section: Fruquintinib: a Novel Anti-vegfr Tkimentioning

confidence: 99%

“…Fruquintinib showed potent inhibition of VEGFR-1, −2 and −3 (half maximal inhibitory concentration [IC 50 ] values were 33 nmol/L, 35 nmol/L and 0.5 nmol/L, respectively), and weak inhibition of RET, FGFR-1 and c-KIT kinases. In addition, fruquintinib also inhibits endothelial cell proliferation and tubule sprouting, thereby preventing tumor angiogenesis 20…”

Section: Pharmacodynamics and Pharmacokineticsmentioning

confidence: 99%

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

Zhang

Zou

Wang

et al. 2019

CMAR

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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.

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Fruquintinib: First Global Approval

Cited by 62 publications

References 9 publications

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

Recent advances on anti-angiogenesis receptor tyrosine kinase inhibitors in cancer therapy

Role of VEGFs/VEGFR-1 Signaling and Its Inhibition in Modulating Tumor Invasion: Experimental Evidence in Different Metastatic Cancer Models

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

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