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    DRUG:

    fexagratinib (ABSK091)

    i
    Other names: ABSK091, AZD4547, AZD 4547, ABSK-091
    Company:
    Abbisko, AstraZeneca
    Drug class:
    pan-FGFR inhib
    Related drugs:
    17d
    Construction of an actin cytoskeleton-related gene signature for predicting prognosis and therapeutic response in glioblastoma: based on machine learning. (PubMed, Transl Cancer Res)
    Drug sensitivity analysis indicated that tozasertib, savolitinib, AZD4547, IWP-2, and GSK591 may have potential therapeutic value. Multi-omics analyses revealed that these key genes are regulated by DNA methylation and transcription factor networks. The actin cytoskeleton-based gene signature serves as an independent indicator of poor prognosis and may support precise prognostic assessment and personalized therapeutic strategies for GBM.
    Journal • Gene Signature
    |
    FGFR1 (Fibroblast growth factor receptor 1) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • EGF (Epidermal growth factor) • PI3K (Phosphoinositide 3-kinases) • PIP5K1A (Phosphatidylinositol-4-Phosphate 5-Kinase Type 1 Alpha)
    |
    PDGFRA mutation
    |
    fexagratinib (ABSK091) • Orpathys (savolitinib) • GSK591 • tozasertib (MK-0457)
    23d
    Stattic enhances the anti-tumor activity of AZD4547 in LUSC by blocking STAT3/RRM2-mediated DNA repair and inducing ROS-driven mitochondrial dysfunction. (PubMed, Cell Death Dis)
    Mechanistically, dual inhibition disrupted the STAT3/RRM2 axis, promoting DNA damage and simultaneously provoking ROS-induced mitochondrial dysfunction. These findings nominate concurrent FGFR1 and STAT3 blockade as a promising therapeutic approach for FGFR1-positive lung squamous cell carcinomas.
    Journal
    |
    FGFR1 (Fibroblast growth factor receptor 1) • IL6 (Interleukin 6) • STAT3 (Signal Transducer And Activator Of Transcription 3) • RRM2 (Ribonucleotide Reductase Regulatory Subunit M2)
    |
    fexagratinib (ABSK091)
    1m
    FGFR2-responsive self-assembled hydrogel releases its inhibitor to suppress the progression of endometriosis. (PubMed, J Control Release)
    In this study, a rationally designed hydrogenator, Nap-Phe-Phe-Phe-Asp-Asp-Asp-Tyr-OH (NapY), was co-assembled with the FGFR2 inhibitor AZD4547 (AZD) to construct an FGFR2-responsive hydrogel, aiming to achieve precise targeted therapy for endometriosis...In vivo studies confirmed that compared with endometriosis model mice treated with free AZD, those treated with Gel Y/AZD exhibited significantly superior inhibitory effects on the growth and metastasis of ectopic lesions. It is anticipated that this research will expect to be applied in the clinical treatment of endometriosis in the near future.
    Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    fexagratinib (ABSK091)
    1m
    National Lung Matrix Trial: Multi-drug Phase II Trial in Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=423, Completed, University of Birmingham | Active, not recruiting --> Completed
    Trial completion • IO biomarker
    |
    NKX2-1 (NK2 Homeobox 1) • TP63 (Tumor protein 63)
    |
    Xalkori (crizotinib) • Tagrisso (osimertinib) • Ibrance (palbociclib) • Imfinzi (durvalumab) • docetaxel • Koselugo (selumetinib) • Truqap (capivasertib) • fexagratinib (ABSK091) • ceralasertib (AZD6738) • sitravatinib (MGCD516) • vistusertib (AZD2014)
    7ms
    Establishment and characterization of preclinical models of human gynecologic tract carcinosarcomas demonstrates targetable FGFR1 alterations. (PubMed, Transl Oncol)
    These findings demonstrate the utility of patient-derived tumor models in the identification and the functional validation of potentially targetable molecular alterations in preclinical setting.
    Preclinical • Journal
    |
    TP53 (Tumor protein P53) • FGFR1 (Fibroblast growth factor receptor 1)
    |
    TP53 mutation
    |
    fexagratinib (ABSK091)
    7ms
    Molecular profiling of ex vivo prostate cancer CAF models captures stromal heterogeneity and drug vulnerabilities. (PubMed, Cell Death Discov)
    CAFs exhibited broad sensitivity to multikinase inhibitors, with dasatinib, midostaurin, and FGFR inhibitors (AZD4547, erdafitinib) emerging as top stromal-directed candidates. These findings underscore the plasticity of prostate CAFs and reveal actionable vulnerabilities, supporting the development of targeted stromal therapies to disrupt tumor-stroma interactions in PCa.
    Preclinical • Journal
    |
    STAT3 (Signal Transducer And Activator Of Transcription 3) • CAV1 (Caveolin 1)
    |
    dasatinib • Balversa (erdafitinib) • midostaurin • fexagratinib (ABSK091)
    8ms
    Development and Validation of a 7-eRNA Prognostic Signature for Lung Adenocarcinoma. (PubMed, Biology (Basel))
    Somatic mutation profiling highlighted TP53 and TTN as frequently mutated genes, while drug sensitivity prediction identified four potential therapeutic agents (including AZD4547 and Nutlin-3a) for high-risk individuals. Collectively, this study constructed a 7-eRNA prognostic model for LUAD, providing a powerful tool for clinical risk assessment and uncovering eRNA-mediated regulatory mechanisms.
    Journal
    |
    TP53 (Tumor protein P53) • TTN (Titin)
    |
    TP53 mutation
    |
    fexagratinib (ABSK091)
    8ms
    Deciphering lactate/lactylation networks in AML: integrated scRNA-seq and transcriptomics reveal functions and prognostic model. (PubMed, BMC Cancer)
    Transcriptomic profiling indicated lactylation-associated immunosuppression (e.g., downregulated CXCL9/10-CXCR3 axis, enrichment of T cell exhaustion markers) and heightened in silico-predicted sensitivity to BCL-2/FGFR inhibitors (ABT-737/AZD4547) in high-risk patients. Collectively, integrated analyses uncovered lactate/lactylation-associated heterogeneity in AML. Our machine learning-based prognostic model predicts survival, therapeutic response, and drug sensitivity, suggesting a potential strategy for precision therapeutics in AML.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • CXCL9 (Chemokine (C-X-C motif) ligand 9) • ARPP19 (CAMP Regulated Phosphoprotein 19) • CXCR3 (C-X-C Motif Chemokine Receptor 3) • IFI16 (Interferon Gamma Inducible Protein 16)
    |
    fexagratinib (ABSK091) • ABT-737
    8ms
    Dual-parameter tomographic imaging of attenuation and backscattering coefficients for quantitative evaluation of immune cell-mediated cytotoxicity in tumor spheroids. (PubMed, Theranostics)
    This approach enables high-resolution measurements of structural and optical property changes associated with apoptosis, allowing spatial and temporal mapping of treatment-induced cytotoxicity in HER2-positive breast tumor spheroids treated with AZD4547 and HER2-targeted chimeric antigen receptor (CAR) T cells... This dual-parameter OCT-based assay framework provides a sensitive, label-free method for distinguishing between immune- and drug-induced apoptosis in tumor spheroids. Its strong correlation with viability and capacity to resolve spatially resolved dynamics underscore its potential for robust, in situ assessment of immunotherapeutic efficacy.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive
    |
    fexagratinib (ABSK091)
    8ms
    NCI-MATCH: Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) (clinicaltrials.gov)
    P2, N=6452, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    MSI (Microsatellite instability) • CD4 (CD4 Molecule)
    |
    Opdivo (nivolumab) • Herceptin (trastuzumab) • Mekinist (trametinib) • Xalkori (crizotinib) • Tagrisso (osimertinib) • Gilotrif (afatinib) • Ibrance (palbociclib) • dasatinib • Tafinlar (dabrafenib) • Vitrakvi (larotrectinib) • sunitinib • Kadcyla (ado-trastuzumab emtansine) • Balversa (erdafitinib) • Mektovi (binimetinib) • adavosertib (AZD1775) • Truqap (capivasertib) • Aliqopa (copanlisib) • fexagratinib (ABSK091) • sapanisertib (CB-228) • ipatasertib (RG7440) • taselisib (GDC-0032) • omipalisib (GSK2126458) • ulixertinib (BVD-523) • Erivedge (vismodegib) • Trazimera (trastuzumab-qyyp) • Fakzynja (defactinib) • GSK2636771 • Paletan (pertuzumab biosimilar) • relatlimab (BMS-986016) • ABP 206 (nivolumab biosimilar) • Pertuvia (pertuzumab biosimilar)
    10ms
    Synergistic Anticancer Effects of Fibroblast Growth Factor Receptor Inhibitor and Cannabidiol in Colorectal Cancer. (PubMed, Nutrients)
    The combination of FGFR inhibitors and cannabidiol exhibited a synergistic effect in inducing cell death in colorectal cancer cells, likely through the ER stress pathway. This study supports the potential of combined FGFR inhibitor and CBD therapy as a promising strategy for enhancing anticancer effects in CRC.
    Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor) • ANXA5 (Annexin A5)
    |
    fexagratinib (ABSK091)
    11ms
    Targeting p-FGFR1Y654 Enhances CD8+ T Cells Infiltration and Overcomes Immunotherapy Resistance in Esophageal Squamous Cell Carcinoma by Regulating the CXCL8-CXCR2 Axis. (PubMed, Biomedicines)
    AZD4547, combined with immunotherapy, further promotes immunotherapeutic efficacy in ESCC. In conclusion, our study presents a promising model for combination therapy in ESCC immunotherapy.
    Journal • IO biomarker
    |
    CD8 (cluster of differentiation 8) • CXCL8 (Chemokine (C-X-C motif) ligand 8) • CXCR2 (Chemokine (C-X-C motif) receptor 2)
    |
    fexagratinib (ABSK091)