^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG CLASS:

FGFR4 inhibitor

12d
Novel FGFR4-Targeting Peptide for Single-Photon Emission Computed Tomography Imaging in Hepatocellular Carcinoma. (PubMed, J Med Chem)
In this study, we designed a series of FGFR4-targeted peptide-radionuclide conjugates (PRCs) based on a high-affinity peptide ligand derived from the binding epitope of the monoclonal antibody U3-1784...In xenograft models, this probe demonstrated high uptake (1.89 ± 0.35% ID/g) and produced high-contrast images specifically in high-FGFR4-expressing tumors. These results indicate that 99mTc-HYNIC-FYQ-8 is a promising peptide-based radiotracer for clinical imaging of FGFR4-overexpressing tumors.
Journal
|
FGFR4 (Fibroblast growth factor receptor 4)
|
U3-1784
13d
Inhibition of neutrophil extracellular traps via the FGF19/ERK/IL-8 axis enhances immune therapy in MSS colorectal cancer. (PubMed, Clin Immunol)
The FGF19/ERK/IL-8 pathway contributed to NET formation in this model. Targeting this pathway represents a promising strategy to boost immunotherapy in MSS CRC.
Journal • PD(L)-1 Biomarker • IO biomarker
|
CD8 (cluster of differentiation 8) • FGF19 (Fibroblast growth factor 19) • FGFR4 (Fibroblast growth factor receptor 4) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
|
BLU 9931
26d
New P2 trial
|
FGF19 (Fibroblast growth factor 19)
|
irpagratinib (ABSK011)
1m
Cytotoxic and senescence-inducing effects of BLU554 in pancreatic ductal adenocarcinoma: an in vitro study. (PubMed, BMC Cancer)
This two-step strategy may represent a novel therapeutic approach for the treatment of therapy-resistant PDAC through senescence induction and subsequent senolysis.
Preclinical • Journal
|
FGFR4 (Fibroblast growth factor receptor 4) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
|
dasatinib • fisogatinib (BLU-554) • BLU 9931
2ms
A Clinical Trial to Evaluate the Relative Bioavailability of New and Old ABSK-011 Capsules (clinicaltrials.gov)
P1, N=40, Completed, Abbisko Therapeutics Co, Ltd | Recruiting --> Completed | N=73 --> 40 | Trial completion date: Dec 2024 --> Sep 2025 | Trial primary completion date: Dec 2024 --> Sep 2025
Trial completion • Enrollment change • Trial completion date • Trial primary completion date
|
irpagratinib (ABSK011) • ABSK061
2ms
Enhancing the antitumor efficacy using a combination of FGFR4 Inhibitor (H3B-6527) and oxaliplatin in gastric cancer. (PubMed, Neoplasia)
These findings indicate that H3B-6527 enhances gastric cancer sensitivity to oxaliplatin by amplifying DNA damage and disrupting cell survival pathways. This study provides a rationale for clinical trials targeting FGFR4 in gastric cancer.
Journal • PARP Biomarker • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • FGFR4 (Fibroblast growth factor receptor 4) • STAT3 (Signal Transducer And Activator Of Transcription 3) • CASP3 (Caspase 3) • CASP7 (Caspase 7)
|
oxaliplatin • H3B-6527
3ms
New P2 trial
3ms
BB102-ST-Ⅰ-02: A Phase 1 Study of BB102 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=78, Recruiting, Broadenbio Ltd., Co. | Trial completion date: Jul 2025 --> Dec 2026 | Trial primary completion date: Jan 2025 --> Dec 2026
Trial completion date • Trial primary completion date
4ms
Reactivation of the PI3K/mTOR Signaling Pathway Confers Resistance to the FGFR4 Inhibitor FGF401. (PubMed, Int J Mol Sci)
The FGF401/everolimus combination effectively suppressed tumor cell proliferation; promoted apoptosis; reduced tumor hypoxia via blood vessel normalization; and downregulated key proteins involved in proliferation, survival, metastasis, and angiogenesis. These preclinical findings provide a strong rationale for clinical trials combining FGFR4 and mTOR inhibitors in HCC patients with FGF19/FGFR4/mTOR-dependent tumors.
Journal
|
FGF19 (Fibroblast growth factor 19) • FGFR4 (Fibroblast growth factor receptor 4)
|
everolimus • roblitinib (FGF401)
4ms
[Expression of Concern] Combination of the FGFR4 inhibitor PD173074 and 5‑fluorouracil reduces proliferation and promotes apoptosis in gastric cancer. (PubMed, Oncol Rep)
The authors were contacted by the Editorial Office to offer an explanation for these apparent anomalies in the presentation of the data in this paper; however, up to this time, no response from them has been forthcoming. Owing to the fact that the Editorial Office has been made aware of potential issues surrounding the scientific integrity of this paper, we are issuing an Expression of Concern to notify readers of this potential problem while the Editorial Office continues to investigate this matter further.  [Oncology Reports 30: 2777‑2784, 2013; DOI: 10.3892/or.2013.2796].
Journal
|
FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4) • GAPDH (Glyceraldehyde-3-Phosphate Dehydrogenase)
|
5-fluorouracil
5ms
Fibroblast growth factor 19-fibroblast growth factor receptor 4 axis: From oncogenesis to targeted-immunotherapy in advanced hepatocellular carcinoma. (PubMed, World J Gastrointest Oncol)
Phase I clinical trials of Irpagratinib (ABSK-011) demonstrated an objective response rate of 43.5%, which increased to 55.6% combined with atezolizumab. It also firstly synthesizes combination strategies and underlying mechanisms between FGFR4 inhibitors and targeted-immunotherapy, addressing critical gaps in existing reviews. Additionally, we discuss the potential of FGF19 as a predictive biomarker, integrating mechanistic and clinical evidence to advance precision HCC therapeutics.
Review • Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1) • FGF19 (Fibroblast growth factor 19) • FGFR4 (Fibroblast growth factor receptor 4)
|
Tecentriq (atezolizumab) • irpagratinib (ABSK011)
6ms
Inhibition of the Caveolin-1 pathway promotes apoptosis and overcomes pan-tyrosine kinase inhibitor resistance in hepatocellular carcinoma. (PubMed, Cell Death Dis)
Combination therapy using either lenvatinib or sorafenib and selective CAV1 inhibitors (e.g., siCAV1/miR-7), or AXL/FGFR4 inhibitors (e.g., BGB324/BLU9931) effectively overcame pan-TKI resistance. Our findings highlight a previously unrecognized role for CAV1-driven signalling in sustaining tumour dormancy, a critical and challenging therapeutic barrier underlying recurrence and pan-TKI resistance in HCC. Therapeutically targeting these pathways offer a promising and novel strategy to eliminate dormant tumour cells, thereby overcoming resistance and improving treatment outcomes.
Journal
|
FGFR4 (Fibroblast growth factor receptor 4) • CDH1 (Cadherin 1) • CAV1 (Caveolin 1) • RAC1 (Rac Family Small GTPase 1) • MIR7 (MicroRNA 7) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
|
sorafenib • Lenvima (lenvatinib) • bemcentinib (BGB324) • BLU 9931