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    over1year
    Anti-tumor efficacy of the novel KIT inhibitor IDRX-42 (formerly M4205) in patient- and cell line-derived xenograft models of gastrointestinal stromal tumor (GIST). (PubMed, Clin Cancer Res)
    IDRX-42 showed significant antitumor activity in patient- and cell line-derived GIST xenograft models. The novel kinase inhibitor induced volumetric responses, decreased mitotic activity and had antiproliferative effects. In models with KIT exon 13 mutation IDRX-42 induced characteristic myxoid degeneration.
    Preclinical • Journal • Stroma
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    PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    KIT mutation • PDGFRA mutation • KIT exon 13 mutation • KIT K642E • KIT D820G • KIT W557
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    imatinib • sunitinib • Ayvakit (avapritinib) • IDRX-42 • M4205
    over2years
    Anti-tumor effects of the novel KIT mutant inhibitor M4205 in gastrointestinal stromal tumor (GIST) xenograft models (ESMO 2022)
    Mice were treated daily with vehicle (control), imatinib (100mg/kg), avapritinib (5mg/kg), sunitinib (20mg/kg), or M4205 (10mg/kg, 25mg/kg). Conclusions M4205 has significant antitumor activity in patient- and cell line-derived GIST xenograft models. The novel kinase inhibitor induces volumetric responses, decreases mitotic activity, has antiproliferative effects and in models with KIT exon 13 mutation leads to characteristic myxoid degeneration.
    Preclinical
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    KIT mutation • PDGFRA mutation • KIT exon 13 mutation • KIT K642E • KIT D820G • KIT W557
    |
    imatinib • sunitinib • Ayvakit (avapritinib) • M4205