Fruzaqla (fruquintinib)

To treat refractory, metastatic colorectal cancer Drug Trials Snapshot

FDA Approval: 11/8/2023

Research Synopsis

  • Fruzaqla (fruquintinib) is an oral selective tyrosine kinase inhibitor approved in China for advanced metastatic colorectal cancer (mCRC), showing promise in treating patients refractory to standard therapies.
  • Recent studies highlight potential cardiovascular risks associated with fruquintinib, including a case of acute aortic dissection in a patient with no prior risk factors, emphasizing the need for careful monitoring for severe side effects.
  • In combination treatments, fruquintinib demonstrated positive outcomes when used alongside raltitrexed and S-1 in a case report, producing a partial response in mCRC patients after previous therapies.
  • A phase 1b/2 clinical trial indicated that combining fruquintinib with sintilimab yielded a response rate of 23.8% in mCRC patients, with promising overall survival statistics.
  • A real-world study compared fruquintinib and regorafenib, revealing fruquintinib had higher objective remission and disease control rates, suggesting it might be a preferred option for treatment in mCRC patients.
  • FRESCO-2, an ongoing phase 3 trial, aims to solidify the efficacy and safety profile of fruquintinib versus placebo in previously treated mCRC patients, contributing to the ongoing research on its therapeutic benefit.
  • New research is exploring the safety profile of fruquintinib in combination with anti-PD-1 antibodies, with studies showing this approach may improve outcomes for patients, especially those with specific mutations.
  • An innovative study involving the sequential delivery of fruquintinib alongside gene therapy strategies demonstrated significant anti-cancer effects, marking a novel direction in combination cancer therapies.
  • Preliminary findings regarding the co-administration of fruquintinib with warfarin indicate a heightened risk of bleeding, necessitating caution due to potential interactions impacting patient safety.
  • Overall, current research indicates fruquintinib represents a promising therapeutic candidate for mCRC, particularly in multi-drug regimens, though further studies are required to confirm safety and efficacy across diverse patient populations.

Related articles

Research articles about Fruzaqla (fruquintinib)

Fruzaqla (fruquintinib)

Acute aortic dissection caused by fruquintinib for metastatic colorectal cancer-a case report and literature review.

London, UK

2 hours ago

1 Received

  • Fruquintinib is a selective tyrosine kinase inhibitor approved in China for treating advanced metastatic colorectal cancer but may cause side effects like hand-foot syndrome and hypertension.
  • A case is reported where a 61-year-old patient, without prior risk factors, developed acute aortic dissection six weeks after starting fruquintinib, suggesting a potential link between the drug and this serious condition.
  • The article highlights the need for healthcare providers to be aware of the cardiovascular risks associated with small-molecule tyrosine kinase inhibitors like fruquintinib and to enhance monitoring and management of such adverse effects.

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Using a combination of fruquintinib, raltitrexed, and S-1 as a third-line treatment for metastatic colorectal cancer with co-existence of Hodgkin lymphoma: a case report.

London, UK

2 hours ago

1 Received

  • * A case report details the treatment journey of a 54-year-old male with mCRC who received combination therapy of fruquintinib, raltitrexed, and S-1 after progressing through previous treatments.
  • * Following the combination treatment, the patient experienced a partial response and continued to have stable disease, highlighting the potential of this regimen in managing late-stage mCRC.

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Phase 1b/2 trial of fruquintinib plus sintilimab in treating advanced solid tumours: The dose-escalation and metastatic colorectal cancer cohort in the dose-expansion phases.

London, UK

2 hours ago

1 Received

  • - This study explored the combination of fruquintinib and sintilimab in patients with advanced solid tumors, particularly focusing on metastatic colorectal cancer (mCRC), showing that the combination is more effective than using either drug alone in preclinical settings.
  • - The research was a multi-center clinical trial that measured safety, tolerability, and early effectiveness, enrolling a total of 60 patients, with some experiencing serious side effects largely related to treatment.
  • - Results indicated that the combination therapy had a 23.8% response rate in mCRC patients, with median progression-free survival of 6.9 months and overall survival of 14.8 months, suggesting a positive trend in treatment efficacy.

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Comparison of the efficacy and safety of fruquintinib and regorafenib in the treatment of metastatic colorectal cancer: A real-world study.

London, UK

2 hours ago

1 Received

  • The study compares the efficacy and safety of fruquintinib and regorafenib for treating metastatic colorectal cancer (mCRC) after standard chemotherapy, using data from 105 patients treated at a hospital in China between 2018 and 2021.
  • Results show that fruquintinib had a higher objective remission rate (6.1% vs 2.0%) and disease control rate (65.3% vs 54.2%) than regorafenib, but both drugs had similar overall survival and progression-free survival rates.
  • When combined with anti-PD-1 therapy, fruquintinib demonstrated significantly better outcomes in both progression-free

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Evaluation of Fruquintinib in the Continuum of Care of Patients with Colorectal Cancer.

London, UK

2 hours ago

1 Received

  • Management of metastatic colorectal cancer (mCRC) involves a continuum of care, primarily utilizing options like trifluridine/tipiracil and regorafenib after patients progress on standard therapies.
  • Fruquintinib, a selective inhibitor for VEGFR-1, -2, and -3, has shown significant anti-tumor effects and was approved for treatment in China based on the successful phase III FRESCO trial.
  • The subsequent FRESCO-2 trial validated these findings in various regions, showing fruquintinib improves overall survival in a heavily pretreated population and highlighting the need for identifying patients who may benefit most from this therapy.

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Case report: Bullous pemphigoid associated with sintilimab therapy for pMMR/MSS colorectal cancer.

London, UK

2 hours ago

1 Received

  • Immunotherapy is an effective cancer treatment but can lead to immune-related adverse events (irAEs), with skin toxicities being the most common.
  • Bullous pemphigoid, a rare but potentially life-threatening skin condition, can occur after immunotherapy treatments like PD-1 inhibitors in colorectal cancer patients.
  • In a reported case, a patient with pMMR/MSS colorectal cancer experienced bullous pemphigoid but improved significantly after treatment, with no new skin lesions and a partial remission of cancer lasting over 8 months.

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Durable responses to tislelizumab plus fruquintinib and radiotherapy in refractory microsatellite stable metastatic colorectal cancer: a case report.

London, UK

2 hours ago

1 Received

  • Immunotherapy is transforming cancer treatment, but microsatellite-stable (MSS) colorectal cancer (CRC) usually doesn't respond well to it compared to microsatellite instability-high CRC.
  • A case study of a young patient with advanced refractory metastatic rectal adenocarcinoma showed promising results after treatment with tislelizumab, fruquintinib, and local radiotherapy, leading to significant health improvements.
  • This case suggests that combining an immune checkpoint inhibitor with an anti-VEGFR-tyrosine kinase inhibitor and local radiation could effectively treat MSS CRC patients who have already undergone extensive treatment.

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Efficacy and safety of toripalimab with fruquintinib in the third-line treatment of refractory advanced metastatic colorectal cancer: results of a single-arm, single-center, prospective, phase II clinical study.

London, UK

2 hours ago

1 Received

  • This study evaluates the effectiveness and safety of the cancer drug fruquintinib combined with the anti-PD-1 antibody toripalimab in treating advanced colorectal cancer patients who do not have microsatellite instability (MSS).
  • A total of 19 MSS patients participated in a clinical trial, where results showed 21.05% had a partial response to treatment, while the median progression-free survival (PFS) was about 6 months.
  • Notably, patients with peritoneal metastasis benefitted the most, experiencing longer PFS compared to others in the study, indicating the potential of this combination therapy for specific patient groups.

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Sequential-delivery nanocomplex for combined anti-angiogenesis and gene therapy against colorectal cancer.

London, UK

2 hours ago

1 Received

  • The study involved co-delivering fruquintinib, an inhibitor of blood vessel growth, and siCCAT1, a small RNA that hinders cancer cell properties, using specially designed nanoparticles that respond to pH changes in the tumor environment.
  • Results showed that this combination not only effectively silenced the target gene but also reduced tumor blood vessel growth, demonstrating significant anti-cancer effects in animal models while maintaining safety and compatibility.

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Oral fruquintinib combined with tegafur-gimeracil-oteracil potassium for advanced colorectal cancer to obtain longer progression-free survival: A case report.

London, UK

2 hours ago

1 Received

  • After standard therapies for metastatic colorectal cancer fail, options are limited and toxicity can impact patient outcomes, highlighting the need for safer treatments.
  • A patient with advanced colorectal cancer experienced successful treatment with fruquintinib, achieving significant progression-free survival and overall treatment duration of over 25.5 months, despite prior treatment interruptions.
  • The case suggests that combining fruquintinib with tegafur-gimeracil-oteracil potassium could lead to improved outcomes in advanced colorectal cancer patients.

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Clinical progress of anti-angiogenic targeted therapy and combination therapy for gastric cancer.

London, UK

2 hours ago

1 Received

  • * The review evaluates the efficacy and safety of various anti-angiogenic targeted drugs (like Ramucirumab and Bevacizumab) for gastric cancer, both as standalone treatments and in combination, based on clinical trial data.
  • * It discusses the challenges of anti-angiogenesis therapy, proposes solutions, and summarizes current clinical research characteristics while providing insights for future studies.

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Case report: long-term sustained remission in a case of metastatic colon cancer with high microsatellite instability and KRAS exon 2 p.G12D mutation treated with fruquintinib after local radiotherapy: a case report and literature review.

London, UK

2 hours ago

1 Received

  • ! The study focuses on the effectiveness of fruquintinib as a treatment after local radiotherapy in a patient with advanced colon cancer characterized by high microsatellite instability and a specific KRAS mutation. * ! After receiving four cycles of pembrolizumab, the patient experienced stable disease, but subsequent combined radiochemical therapy showed limited results. * ! The administration of fruquintinib led to sustained partial remission, with the patient remaining in continuous remission for 30 months at the last follow-up, suggesting it may be a viable treatment option for certain metastatic colorectal cancer patients. * !

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DC101, an anti-VEGFR2 agent, promotes high-endothelial venule formation and immune infiltration versus SAR131675 and fruquintinib.

London, UK

2 hours ago

1 Received

  • There is growing interest in combining immune checkpoint inhibitors (ICIs) with anti-angiogenic drugs to improve cancer treatment, specifically focusing on three agents: DC101, SAR131675, and fruquintinib.
  • In a study conducted on melanoma in mice, both DC101 and fruquintinib showed significant effectiveness in slowing tumor growth and increasing immune cell infiltration, especially DC101, which had stronger effects on T cell activity and tumor microenvironment changes.
  • The results suggest that DC101 is potentially a better option for future clinical combinations with ICIs due to its greater impact on immune responses and tumor characteristics compared to the other agents tested.

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Fruquintinib versus placebo in patients with refractory metastatic colorectal cancer (FRESCO-2): an international, multicentre, randomised, double-blind, phase 3 study.

London, UK

2 hours ago

1 Received

  • The study aimed to assess the effectiveness and safety of fruquintinib, an oral drug targeting vascular endothelial growth factor receptors, in patients with advanced colorectal cancer who had not responded to existing treatments.
  • Conducted as a phase 3 clinical trial (FRESCO-2) across 14 countries, the research involved 691 patients randomly assigned to receive either fruquintinib or a placebo in addition to supportive care.
  • The primary goal was to measure overall survival, and the study is currently ongoing with results being analyzed following the occurrence of 480 patient deaths.

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Durable responses to TAS-102 plus bevacizumab and TACE in salvage-line treatment of KRAS-mutated and MSS metastatic colorectal cancer: a case report.

London, UK

2 hours ago

1 Received

  • * A case study reports significant success in a patient receiving a fifth-line treatment of TAS-102, bevacizumab, and transcatheter arterial chemoembolization (TACE) after failing standard treatments.
  • * The patient experienced a progression-free survival (PFS) of over 11.6 months, with reduced tumor markers, improved symptoms, and quality of life, indicating this combination may be an effective option for similar cases.

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Angiogenesis inhibition in metastatic colorectal cancer continuum of care.

London, UK

2 hours ago

1 Received

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A2AR-mediated lymphangiogenesis via VEGFR2 signaling prevents salt-sensitive hypertension.

London, UK

2 hours ago

1 Received

  • Excess sodium intake contributes to hypertension through lymphatic dysfunction, with a focus on the role of the adenosine A2A receptor (A2AR) in lymphatic endothelial cells (LECs) during salt-induced hypertension.* -
  • Mice with LEC-specific knockout of A2AR showed higher blood pressure and decreased lymphatic density, while A2AR activation using an agonist improved lymphatic density and lowered blood pressure, indicating its importance in regulating lymphatic function.* -
  • The findings suggest A2AR-mediated signaling promotes lymphangiogenesis and sodium balance independently of VEGF, pointing to its potential as a therapeutic target for managing salt-sensitive hypertension.*

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Design, synthesis and biological evaluation of VEGFR-2/HDAC dual inhibitors as multitargeted antitumor agents based on fruquintinib and vorinostat.

London, UK

2 hours ago

1 Received

  • A new series of compounds called 4-(benzofuran-6-yloxy)quinazoline derivatives were created as dual inhibitors targeting VEGFR-2 and HDAC, inspired by existing drugs fruquintinib and vorinostat.
  • Among these compounds, compound 13 showed strong inhibitory effects on VEGFR-2 and HDAC1, with impressive antiproliferative activity against various cancer cell lines like MCF-7 and HeLa.
  • Compound 13 slowed down cell growth during specific cell cycle phases and caused significant cell death in HeLa cells, while also demonstrating anti-angiogenic effects, making it a promising candidate for further cancer treatment research.

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Anlotinib and fruquintinib co-administrated with warfarin increases the risk of bleeding: Studied from pharmacokinetic and pharmacodynamic perspectives.

London, UK

2 hours ago

1 Received

  • - Recent studies highlight a concerning risk of bleeding when combining vascular endothelial growth factor receptor tyrosine kinase inhibitors (VEGFR-TKIs) like anlotinib and fruquintinib with the anticoagulant warfarin, particularly affecting patients at risk for deep vein thrombosis (DVT).
  • - Research investigated how anlotinib and fruquintinib influence warfarin's pharmacokinetics and pharmacodynamics using rat models, revealing anlotinib significantly inhibits enzymes that metabolize warfarin, increasing its blood concentration and enhancing its anticoagulant effects.
  • - The findings suggest that while anlotinib increases the efficacy of warfarin, leading to better outcomes

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