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    DRUG:

    MRTX0902

    i
    Other names: MRTX0902, MRTX 0902, MRTX-0902
    Associations

    News

    Trials
    Company:
    BMS
    Drug class:
    SOS1 inhibitor
    Related drugs:
    Associations

    News

    Trials
    7d
    Characterization of the BH1406 non-small cell lung cancer (NSCLC) cell line carrying an activating SOS1 mutation. (PubMed, Transl Lung Cancer Res)
    Besides BAY-293, BH1406 cells proved to be sensitive to the SOS1 inhibitors MRTX0902 and BI-3406...Additionally, the PI3K inhibitor dactolisib, the GSK-3 inhibitor BI-5521 as well as the bromodomain protein-directed PROTAC ARV-771 inhibited the growth of BH1406 cells significantly and showed synergistic interaction with BAY-293...BH1406 cells represent a novel cellular model suitable for the molecular characterization of SOS1 druggability. Such rare oncogenic driver genes are not included in standard NGS panels and need to be detected by expanded assays like WES.
    Preclinical • Journal
    |
    CHEK2 (Checkpoint kinase 2) • STAT3 (Signal Transducer And Activator Of Transcription 3) • SOS1 (SOS Ras/Rac Guanine Nucleotide Exchange Factor 1)
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    MYC expression
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    Lung Cancer Mutation Panel
    |
    dactolisib (RTB101) • BI-3406 • MRTX0902
    6ms
    The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading. (PubMed, Mol Cancer Ther)
    MRTX0902 augmented the antitumor activity of the KRAS G12C inhibitor adagrasib when dosed in combination in eight out of 12 KRAS G12C-mutant human non-small cell lung cancer and colorectal cancer xenograft models. Lastly, combined vertical inhibition of RTK/MAPK pathway signaling by MRTX0902 with inhibitors of EGFR or RAF/MEK led to greater downregulation of pathway signaling and improved antitumor responses in KRAS-MAPK pathway-mutant models. These studies demonstrate the potential clinical application of dual inhibition of SOS1 and KRAS G12C and additional SOS1 combination strategies that will aide in the understanding of SOS1 and RTK/MAPK biology in targeted cancer therapy.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • PTEN (Phosphatase and tensin homolog) • NF1 (Neurofibromin 1)
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    Krazati (adagrasib) • MRTX0902
    8ms
    The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading. (PubMed, Mol Cancer Ther)
    MRTX0902 augmented the antitumor activity of the KRAS G12C inhibitor adagrasib when dosed in combination in eight out of twelve KRAS G12C-mutant human non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) xenograft models. Lastly, combined vertical inhibition of RTK/MAPK pathway signaling by MRTX0902 with inhibitors of EGFR or RAF/MEK led to greater downregulation of pathway signaling and improved antitumor responses in KRAS-MAPK pathway-mutant models. These studies demonstrate the potential clinical application of dual inhibition of SOS1 and KRAS G12C and additional SOS1 combination strategies that will aide in the understanding of SOS1 and RTK/MAPK biology in targeted cancer therapy.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • PTEN (Phosphatase and tensin homolog) • NF1 (Neurofibromin 1)
    |
    KRAS mutation
    |
    Krazati (adagrasib) • MRTX0902
    2years
    A Phase 1/2 Study of MRTX0902 in Solid Tumors With Mutations in the KRAS MAPK Pathway (clinicaltrials.gov)
    P1/2, N=225, Recruiting, Mirati Therapeutics Inc. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
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    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • NF1 (Neurofibromin 1) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
    |
    KRAS mutation • EGFR mutation • KRAS G12C • NF1 mutation • KRAS G12
    |
    Krazati (adagrasib) • MRTX0902
    2years
    A Phase 1/2 Study of MRTX0902 in Solid Tumors With Mutations in the KRAS MAPK Pathway (clinicaltrials.gov)
    P1/2, N=225, Not yet recruiting, Mirati Therapeutics Inc.
    New P1/2 trial • Metastases
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • NF1 (Neurofibromin 1) • PTPN11 (Protein Tyrosine Phosphatase Non-Receptor Type 11)
    |
    KRAS mutation • EGFR mutation • KRAS G12C • NF1 mutation • KRAS G12
    |
    Krazati (adagrasib) • MRTX0902