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    DRUG:

    IPN60090

    i
    Other names: IPN60090, IACS-6274
    Company:
    Ipsen, UT MD Anderson Cancer Center
    Drug class:
    Glutaminase inhibitor
    Related drugs:
    2ms
    Glutaminase 1 plays critical roles in myelodysplastic syndrome and acute myeloid leukemia cells. (PubMed, Cancer Biomark)
    The efficacy of GLS inhibitors (CB839 or IPN60090) and BCL2 inhibitor venetoclax was also examined. Cells transfected with GLS1 short hairpin RNA showed suppressed proliferation under hypoxic conditions and increased sensitivity to venetoclax. Targeting glutaminolysis and BCL2 inhibition enhances the therapeutic efficacy and has been proposed as a novel strategy for treating high-risk MDS and AML.
    Journal • IO biomarker
    |
    GLS1 (Glutaminase) • GLS2 (Glutaminase 2)
    |
    Venclexta (venetoclax) • IPN60090 • telaglenastat (CB-839)
    1year
    IACS-6274 With or Without Bevacizumab and Paclitaxel for the Treatment of Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=54, Recruiting, M.D. Anderson Cancer Center | N=84 --> 54
    Enrollment change • Metastases
    |
    PD-L1 (Programmed death ligand 1) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • STK11 (Serine/threonine kinase 11) • ARID1A (AT-rich interaction domain 1A) • NF1 (Neurofibromin 1) • KEAP1 (Kelch Like ECH Associated Protein 1) • PD-1 (Programmed cell death 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
    |
    PIK3CA mutation • PTEN mutation • ARID1A mutation • STK11 mutation • NF1 mutation • KEAP1 mutation • NFE2L2 mutation • PIK3CA mutation + PTEN mutation
    |
    Avastin (bevacizumab) • paclitaxel • Truqap (capivasertib) • IPN60090
    1year
    Aspirin and the metabolic hallmark of cancer: novel therapeutic opportunities for colorectal cancer. (PubMed, Explor Target Antitumor Ther)
    Importantly, as aspirin treatment exposes metabolic vulnerabilities in tumour cells, there is an opportunity for the use of aspirin in combination with specific metabolic inhibitors in particular, glutaminase (GLS) inhibitors currently in clinical trials such as telaglenastat (CB-839) and IACS-6274 for the treatment of colorectal and potentially other cancers. The increasing evidence that aspirin impacts metabolism in cancer cells suggests that aspirin could provide a simple, relatively safe, and cost-effective way to target this important hallmark of cancer. Excitingly, this review highlights a potential new role for aspirin in improving the efficacy of a new generation of metabolic inhibitors currently undergoing clinical investigation.
    Review • Journal
    |
    mTOR (Mechanistic target of rapamycin kinase)
    |
    IPN60090 • telaglenastat (CB-839) • aspirin
    1year
    A Novel Glutaminase 1 Inhibitor (IACS-6274) Radiosensitizes Mutant KEAP1 Lung Cancer Models to Photons and Protons (ASTRO 2023)
    No abstract available
    Preclinical
    |
    KEAP1 (Kelch Like ECH Associated Protein 1)
    |
    KEAP1 mutation
    |
    IPN60090
    over1year
    IACS-6274 With or Without Bevacizumab and Paclitaxel for the Treatment of Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=84, Recruiting, M.D. Anderson Cancer Center | N=36 --> 84
    Enrollment change • Metastases
    |
    PD-L1 (Programmed death ligand 1) • STK11 (Serine/threonine kinase 11) • ARID1A (AT-rich interaction domain 1A) • NF1 (Neurofibromin 1) • KEAP1 (Kelch Like ECH Associated Protein 1) • PD-1 (Programmed cell death 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
    |
    ARID1A mutation • STK11 mutation • NF1 mutation • KEAP1 mutation • NFE2L2 mutation
    |
    Avastin (bevacizumab) • paclitaxel • IPN60090
    2years
    IACS-6274 With or Without Pembrolizumab for the Treatment of Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=36, Recruiting, M.D. Anderson Cancer Center | Initiation date: Feb 2022 --> Sep 2021
    Trial initiation date
    |
    PD-L1 (Programmed death ligand 1) • STK11 (Serine/threonine kinase 11) • ARID1A (AT-rich interaction domain 1A) • NF1 (Neurofibromin 1) • KEAP1 (Kelch Like ECH Associated Protein 1) • PD-1 (Programmed cell death 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
    |
    ARID1A mutation • STK11 mutation • NF1 mutation • KEAP1 mutation • NFE2L2 mutation
    |
    Keytruda (pembrolizumab) • IPN60090
    over2years
    THE PIVOTAL ROLE OF GLUTAMINOLYSIS IN MYELODYSPLASTIC SYNDROME (MDS): A NOVEL STRATEGY FOR THE TARGETED THERAPY OF MDS (EHA 2022)
    We also investigated the efficacy of GLS inhibitor (CB-839 or IPN-60090) and BCL2 inhibitor, venetoclax by using MDS and AML cell line, SKM-1, MDS-L, MOLM-14, THP-1, MV4;11 and osteoblastic cell line, MC3T3-E1. Conclusion Targeting of glutaminolysis and BCL2 inhibition combine to enhance therapeutic efficacy and has been proposed as a novel strategy high-risk MDS and AML. We also provide the promising clinical relevance as a candidate drug for treatment of MDS and AML patients.
    IO biomarker
    |
    CASP3 (Caspase 3) • CASP7 (Caspase 7) • GLS1 (Glutaminase) • GLS2 (Glutaminase 2)
    |
    Venclexta (venetoclax) • IPN60090 • telaglenastat (CB-839)
    3years
    IACS-6274 With or Without Pembrolizumab for the Treatment of Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=36, Recruiting, M.D. Anderson Cancer Center
    Clinical • New P1 trial
    |
    PD-L1 (Programmed death ligand 1) • STK11 (Serine/threonine kinase 11) • ARID1A (AT-rich interaction domain 1A) • NF1 (Neurofibromin 1) • KEAP1 (Kelch Like ECH Associated Protein 1) • PD-1 (Programmed cell death 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
    |
    ARID1A mutation • STK11 mutation • NF1 mutation • KEAP1 mutation • NFE2L2 mutation
    |
    Keytruda (pembrolizumab) • IPN60090
    over3years
    [VIRTUAL] Integrated approach towards defining mechanism based combinations to guide clinical development of glutaminase inhibitors (AACR 2021)
    IPN60090, dosed in combination with inhibitors of these pathways yields regressions and off-treatment, durable responses in preclinical models of KEAP1-mutant NSCLC. Based on these data, combination strategies are being developed for Phase 1b expansion cohorts.
    Clinical
    |
    KEAP1 (Kelch Like ECH Associated Protein 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
    |
    KEAP1 mutation • NFE2L2 mutation
    |
    IPN60090
    over4years
    [VIRTUAL] IPN60090: A potent and selective inhibitor of glutaminase being developed for KEAP1/NFE2L2 mutant NSCLC and ASNS-low HGSOC patients (AACR-I 2020)
    IPN60090: A potent and selective inhibitor of glutaminase being developed for KEAP1/NFE2L2 mutant NSCLC and ASNS-low HGSOC patients
    Clinical
    |
    KEAP1 (Kelch Like ECH Associated Protein 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2)
    |
    KEAP1 mutation • NFE2L2 mutation
    |
    IPN60090