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    DRUG:

    tinodasertib (AUM001)

    i
    Other names: AUM001, ETC-206, ETC-1907206
    Associations

    News

    Trials
    Company:
    AUM Biosci, Experimental Therapeutics Centre, Newsoara Biopharma
    Drug class:
    MKNK1 inhibitor, MKNK2 inhibitor
    Related drugs:
    Associations

    News

    Trials
    5ms
    Reversal of ABCG2-mediated drug resistance by tinodasertib (ETC-206). (PubMed, Front Pharmacol)
    In monolayer cultures, co-administration of tinodasertib significantly sensitized ABCG2-overexpressing cells to mitoxantrone and topotecan. The concordance between ATPase inhibition and in silico docking supports a model wherein tinodasertib occupies the substrate-binding pocket of ABCG2, preventing ATP hydrolysis and subsequent drug transport. Overall, combining tinodasertib with ABCG2 substrate chemotherapeutics may represent a promising strategy for overcoming MDR in tumors overexpressing ABCG2, warranting further in vivo validation and clinical evaluation.
    Journal
    |
    ABCG2 (ATP Binding Cassette Subfamily G Member 2)
    |
    mitoxantrone • topotecan • tinodasertib (AUM001)
    almost2years
    MNK Inhibitor AUM001 in Combination With Either Pembrolizumab or Irinotecan to Treat Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=120, Recruiting, AUM Biosciences Pte Ltd | Trial primary completion date: Aug 2023 --> Sep 2024
    Trial primary completion date • Combination therapy • Metastases
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    BRAF V600E • MSI-H/dMMR • BRAF V600
    |
    Keytruda (pembrolizumab) • irinotecan • tinodasertib (AUM001)
    over2years
    MNK Inhibitor AUM001 in Combination With Either Pembrolizumab or Irinotecan to Treat Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=120, Recruiting, AUM Biosciences Pte Ltd | Not yet recruiting --> Recruiting | Initiation date: Oct 2022 --> Apr 2023
    Enrollment open • Trial initiation date • Combination therapy • Metastases
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    BRAF V600E • MSI-H/dMMR • BRAF V600
    |
    Keytruda (pembrolizumab) • irinotecan • tinodasertib (AUM001)
    over3years
    MNK Inhibitor AUM001 in Combination With Either Pembrolizumab or Irinotecan to Treat Metastatic Colorectal Cancer (clinicaltrials.gov)
    P2, N=120, Not yet recruiting, AUM Biosciences Pte Ltd
    New P2 trial • Combination therapy
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    BRAF V600E • MSI-H/dMMR • BRAF V600
    |
    Keytruda (pembrolizumab) • irinotecan • tinodasertib (AUM001)