ArticleCancer biology & therapy2014
Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy.
Article in Cancer biology & therapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05168527 (An Open Single-center Phase II Clinical Study of Fruquintinib Combined With Chemotherapy in Patients With Liver Metastases From Pancreatic Cancer), which is not on this map. Cited by 88 papers, 4 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
An Open Single-center Phase II Clinical Study of Fruquintinib Combined With Chemotherapy in Patients With Liver Metastases From Pancreatic Cancer
Who cites it
88 citing papers in PubMed, 4 syntheses or guidelines pooled it, 151 citations in OpenAlex.
- The efficacy and safety of regorafenib/fruquintinib combined with PD-1/PD-L1 for metastatic colorectal cancer: a meta-analysis based on single-arm studies.Frontiers in immunology · 2025Pooled it
- Efficacy and safety of fruquintinib in the treatment of colorectal cancer: a systematic review and meta-analysis of studies in China.Frontiers in pharmacology · 2025Pooled it
- Clinical research progress of fruquintinib in the treatment of malignant tumors.Investigational new drugs · 2024Pooled it
- A comparison of regorafenib and fruquintinib for metastatic colorectal cancer: a systematic review and network meta-analysis.Journal of cancer research and clinical oncology · 2019Pooled it
- Matching-adjusted indirect comparison of fruquintinib versus ramucirumab in advanced gastric or gastroesophageal junction adenocarcinoma.Journal of comparative effectiveness research · 2026Trial
- Efficacy and safety of fruquintinib combined with albumin-bound paclitaxel as second-line therapy for advanced gastric cancer following failure of PD-1 inhibitor-containing treatment (TACTIC GC-01): A phase II single-arm study.International journal of cancer · 2026Trial
- Fruquintinib Plus TAS-102 With or Without SBRT as Third- Or Later-Line Therapy for Metastatic Colorectal Cancer: Preliminary Results From a Prospective Phase II Trial.Cancer medicine · 2026Trial
- Assessment of the Effects of Fruquintinib on Cardiac Safety in Patients with Metastatic Colorectal Cancer.Journal of clinical pharmacology · 2025Trial
- Efficacy and safety of fruquintinib in patients with refractory metastatic colorectal cancer: a FRESCO-2 subgroup analysis of patients enrolled in Japan.International journal of clinical oncology · 2025Trial
- Population Pharmacokinetics of Fruquintinib, a Selective Oral Inhibitor of VEGFR -1, -2, and -3, in Patients with Refractory Metastatic Colorectal Cancer.Journal of clinical pharmacology · 2025Trial
- Fruquintinib versus placebo in patients with refractory metastatic colorectal cancer: safety analysis of FRESCO-2.The oncologist · 2025Trial
- Assessment of Food Effect and pH-Dependent Drug-Drug Interactions of Fruquintinib in Healthy Subjects.Clinical and translational science · 2025Trial
- Fruquintinib plus paclitaxel versus placebo plus paclitaxel for gastric or gastroesophageal junction adenocarcinoma: the randomized phase 3 FRUTIGA trial.Nature medicine · 2024Trial
- Efficacy and safety of fruquintinib dose-escalation strategy for elderly patients with refractory metastatic colorectal cancer: A single-arm, multicenter, phase II study.Cancer medicine · 2023Trial
- Trial
- Safety and efficacy of fruquintinib in patients with previously treated metastatic colorectal cancer: a phase Ib study and a randomized double-blind phase II study.Journal of hematology & oncology · 2017Trial
- Real-world efficacy, safety, and treatment continuity of fruquintinib in Japanese patients with colorectal cancer: a multicentre retrospective study.ESMO gastrointestinal oncology · 2026Article
- Article
- Fruquintinib: Mechanism of Action, Clinical, and Translational Science.Clinical and translational science · 2026Review
- Real-world efficacy and safety of fruquintinib plus PD-1 inhibitors with or without radiotherapy in refractory metastatic colorectal cancer: a single-center retrospective cohort study.Journal of gastrointestinal oncology · 2026Article
28 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
23 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
VEGF/VEGFR signal axis has been proven to be an important target for development of novel cancer therapies. One challenging aspect in small molecular VEGFR inhibitors is to achieve sustained target inhibition at tolerable doses previously seen only with the long-acting biologics. It would require high potency (low effective drug concentrations) and sufficient drug exposures at tolerated doses so that the drug concentration can be maintained above effective drug concentration for target inhibition within the dosing period. Fruquintinib (HMPL-013) is a small molecule inhibitor with strong potency and high selectivity against VEGFR family currently in Phase II clinical studies. Analysis of Phase I pharmacokinetic data revealed that at the maximum tolerated dose of once daily oral administration fruquintinib achieved complete VEGFR2 suppression (drug concentrations were maintained above that required to produce >85% inhibition of VEGFR2 phosphorylation in mouse) for 24 hours/day. In this article, the preclinical data for fruquintinib will be described, including kinase enzyme activity and selectivity, cellular VEGFR inhibition and VEGFR-driven functional activity, in vivo VEGFR phosphorylation inhibition in the lung tissue in mouse and tumor growth inhibition in a panel of tumor xenograft and patient derive xenograft models in mouse. Pharmacokinetic and target inhibition data are also presented to provide a correlation between target inhibition and tumor growth inhibition.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.