^
    8ms
    A First-in-human (FIH) Study of IDRX-42 in Participants With Metastatic and/or Unresectable Gastrointestinal Stromal Tumors (GIST) [Study ID: StrateGIST 1] (clinicaltrials.gov)
    P1, N=240, Recruiting, IDRx, Inc. | N=143 --> 240
    Enrollment change • Stroma • Metastases
    |
    PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    KIT mutation • PDGFRA mutation • PDGFRA exon 18 mutation
    |
    sunitinib • IDRX-42
    10ms
    KIT/PDGFRA inhibitors for the treatment of gastrointestinal stromal tumors: getting to the gist of the problem. (PubMed, Expert Opin Investig Drugs)
    Despite the outstanding results of first-line imatinib in advanced GIST, resistance ultimately occurs mainly through secondary mutations in KIT/PDGFRA...However, it is now recognized that the situation is more intricate, with various factors interacting with KIT and PDGFRA, playing a crucial role in the response and resistance to treatments. Future strategies in the management of advanced GIST should integrate driver inhibition with the blockade of other molecules to enhance cell death and establish enduring responses in patients.
    Journal • Stroma
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    KIT mutation • PDGFRA mutation
    |
    imatinib • Ayvakit (avapritinib) • Qinlock (ripretinib) • IDRX-42 • bezuclastinib (PLX9486)
    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
    |
    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) • IDRX-42 • M4205
    over2years
    ANTI-TUMOR EFFECTS OF THE NOVEL KIT MUTANT INHIBITOR M4205/IDRX-42 IN GASTROINTESTINAL STROMAL TUMOR (GIST) XENOGRAFT MODELS (CTOS 2022)
    No abstract available
    Preclinical
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase)
    |
    IDRX-42
    over2years
    FIRST-IN-HUMAN PHASE 1/1B STUDY OF IDRX-42, A NOVEL ORAL TYROSINE KINASE KIT INHIBITOR, IN PARTICIPANTS WITH METASTATIC AND/OR UNRESECTABLE GASTROINTESTINAL STROMAL TUMORS (CTOS 2022)
    Objective: The majority of gastrointestinal stromal tumors (GISTs) are driven by constitutively activated kinases, either KIT or PDGFRA, and respond to treatment with tyrosine kinase inhibitors (TKI) such as imatinib, sunitinib, regorafenib, and ripretinib. Not applicable
    P1 data
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    KIT mutation • PDGFRA mutation • PDGFRA exon 18 mutation
    |
    imatinib • sunitinib • Stivarga (regorafenib) • Qinlock (ripretinib) • IDRX-42
    over2years
    A First-in-human (FIH) Study of IDRX-42 in Participants With Metastatic and/or Unresectable Gastrointestinal Stromal Tumors (clinicaltrials.gov)
    P1, N=143, Recruiting, IDRx, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    KIT mutation • PDGFRA mutation • PDGFRA exon 18 mutation
    |
    sunitinib • IDRX-42
    over2years
    A First-in-human (FIH) Study of IDRX-42 in Participants With Metastatic and/or Unresectable Gastrointestinal Stromal Tumors (clinicaltrials.gov)
    P1, N=143, Not yet recruiting, IDRx, Inc.
    New P1 trial
    |
    PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    KIT mutation • PDGFRA mutation • PDGFRA exon 18 mutation
    |
    sunitinib • IDRX-42