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

    elraglusib (9-ING-41)

    i
    Other names: 9-ING-41, 9 ING 41, 9ING41
    Company:
    Actuate Therap
    Drug class:
    GSK3β inhibitor
    Related drugs:
    8d
    Drug Repurposing for AML: Structure-Based Virtual Screening and Molecular Simulations of FDA-Approved Compounds with Polypharmacological Potential. (PubMed, Biomedicines)
    While targeted agents-such as LSD1 inhibitors, the BCL-2 inhibitor venetoclax, and IDH1 inhibitors-have provided clinical benefit, their efficacy is often limited by compensatory signaling and clonal evolution. This computational study supports the feasibility of a polypharmacology-based strategy for AML therapy by integrating epigenetic modulation, apoptotic reactivation, and metabolic correction within single molecular scaffolds. However, the identified compounds (Belumosudil, DB08512, and Elraglusib) have not yet demonstrated efficacy in AML models; further preclinical validation is warranted to substantiate these predictions and advance translational development.
    FDA event • Journal • IO biomarker
    |
    IDH1 (Isocitrate dehydrogenase (NADP(+)) 1)
    |
    IDH1 mutation • IDH1 R132
    |
    Venclexta (venetoclax) • elraglusib (9-ING-41)
    5ms
    9-ING-41 in Pediatric Patients With Refractory Malignancies. (clinicaltrials.gov)
    P1, N=40, Terminated, Actuate Therapeutics Inc. | N=68 --> 40 | Trial completion date: Dec 2024 --> Jul 2025 | Recruiting --> Terminated | Trial primary completion date: Dec 2024 --> Jul 2025; The decision to conclude study was made to optimize the clinical study design and protocol to further evaluate the safety profile of elraglusib (9-ING-41) in pediatric and adult patients with refractory Ewings Sarcoma.
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    |
    AFP (Alpha-fetoprotein)
    |
    temozolomide • cyclophosphamide • irinotecan • topotecan • elraglusib (9-ING-41)
    1year
    Targeted inhibition of glycogen synthase kinase-3 using 9-ING-41 (elraglusib) enhances CD8 T-cell-reactivity against neuroblastoma cells. (PubMed, Sci Rep)
    Finally, in co-culture experiments with CD8 + T cells, 9-ING-41 improved immune recognition of the neuroblastoma cells, as evidenced by augmented T-cell activation marker levels and T-cell proliferation, which was further enhanced by PD-1 immune checkpoint inhibition. Our preclinical study provides experimental support to further explore the GSK-3β inhibitor 9-ING-41 as an immunomodulatory agent to increase tumor immune recognition in neuroblastoma.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    CD8 (cluster of differentiation 8) • MYCN (MYCN Proto-Oncogene BHLH Transcription Factor)
    |
    MYCN amplification
    |
    elraglusib (9-ING-41)
    1year
    A New Strategy for Adult T-Cell Leukemia Treatment Targeting Glycogen Synthase Kinase-3β. (PubMed, Eur J Haematol)
    GSK-3β functions as an oncogene in ATL and could be a potential therapeutic target.
    Journal
    |
    TP53 (Tumor protein P53) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1) • BCL2L1 (BCL2-like 1) • STAT3 (Signal Transducer And Activator Of Transcription 3) • BIRC5 (Baculoviral IAP repeat containing 5) • BAX (BCL2-associated X protein) • CCNA2 (Cyclin A2) • XIAP (X-Linked Inhibitor Of Apoptosis) • CDK1 (Cyclin-dependent kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • GSK3B (Glycogen Synthase Kinase 3 Beta) • NFKBIA (NFKB Inhibitor Alpha 2) • BAK1 (BCL2 Antagonist/Killer 1) • JUNB (JunB Proto-Oncogene AP-1 Transcription Factor Subunit)
    |
    MYC expression • MCL1 expression • TP53 expression • BIRC5 expression • BAX expression • CDKN1B expression
    |
    elraglusib (9-ING-41) • LY2090314
    over1year
    9-ING-41 in Pediatric Patients With Refractory Malignancies. (clinicaltrials.gov)
    P1, N=68, Recruiting, Actuate Therapeutics Inc. | Active, not recruiting --> Recruiting
    Enrollment open
    |
    AFP (Alpha-fetoprotein)
    |
    temozolomide • cyclophosphamide • irinotecan • topotecan • elraglusib (9-ING-41)
    over1year
    Mutational analysis of cfDNA to identify predictive biomarkers in previously untreated patients with metastatic pancreatic cancer receiving the GSK-3 inhibitor elraglusib (9-ING-41) in combination with gemcitabine/nab-paclitaxel in the 1801 phase 2 study. (ASCO 2024)
    Our preliminary analysis of gene mutations in liquid biopsy samples obtained from patients in the ongoing 1801 Part 3B phase 2 trial identified potential predictive biomarkers of clinical outcome in mPDAC patients treated with combination of elraglusib/GnP. Clinical trial information: NCT03678883.
    Combination therapy • P2 data • Clinical • Metastases • Cell-free DNA
    |
    KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • DNMT3A (DNA methyltransferase 1) • NOTCH1 (Notch 1) • KMT2C (Lysine Methyltransferase 2C) • NOTCH2 (Notch 2)
    |
    Tempus xF+ Panel
    |
    gemcitabine • albumin-bound paclitaxel • elraglusib (9-ING-41)
    over1year
    9-ING-41 Plus Carboplatin in Salivary Gland Carcinoma (clinicaltrials.gov)
    P2, N=35, Active, not recruiting, Glenn J. Hanna | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    carboplatin • elraglusib (9-ING-41)
    over1year
    FOLFIRINOX + 9-Ing-41 + Losartan In Pancreatic Cancer (clinicaltrials.gov)
    P2, N=70, Recruiting, Colin D. Weekes, M.D., PhD | Trial completion date: Jul 2024 --> Jul 2026 | Trial primary completion date: Dec 2023 --> Dec 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium • elraglusib (9-ING-41)
    almost2years
    Actuate 1901: 9-ING-41 in Myelofibrosis (clinicaltrials.gov)
    P2, N=17, Completed, Actuate Therapeutics Inc. | Active, not recruiting --> Completed
    Trial completion
    |
    Jakafi (ruxolitinib) • elraglusib (9-ING-41)
    almost2years
    Actuate 1801: 9-ING-41 in Patients With Advanced Cancers (clinicaltrials.gov)
    P2, N=350, Active, not recruiting, Actuate Therapeutics Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    carboplatin • gemcitabine • albumin-bound paclitaxel • irinotecan • pegylated liposomal doxorubicin • lomustine • elraglusib (9-ING-41)
    almost2years
    Actuate 1801: 9-ING-41 in Patients With Advanced Cancers (clinicaltrials.gov)
    P2, N=350, Recruiting, Actuate Therapeutics Inc.
    Trial completion date • Trial primary completion date • Metastases
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    carboplatin • gemcitabine • albumin-bound paclitaxel • irinotecan • pegylated liposomal doxorubicin • lomustine • elraglusib (9-ING-41)
    almost2years
    9-ING-41 Plus Carboplatin in Salivary Gland Carcinoma (clinicaltrials.gov)
    P2, N=35, Recruiting, Glenn J. Hanna | Trial primary completion date: Jan 2024 --> Jun 2024
    Trial primary completion date • Metastases
    |
    carboplatin • elraglusib (9-ING-41)