^
    10ms
    A first-in-human phase I trial of NB003, a potent and selective KIT/PDGFRa inhibitor, in patients with advanced gastrointestinal stromal tumors (GIST) (ESMO 2023)
    Conclusions NB003 has a manageable toxicity profile and promising clinical activity in heavily pretreated pts with advanced GIST harboring a broad spectrum of acquired imatinib-resistant mutations. The 20mg and 30mg BID doses are selected for further investigation in the phase I RP2D confirmation cohort.
    Clinical • P1 data • Stroma • Metastases
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    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
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    KIT mutation
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    imatinib • NB003
    almost3years
    A Study of NB003 in Patients With Advanced Malignancies (clinicaltrials.gov)
    P1, N=36, Recruiting, Ningbo Newbay Technology Development Co., Ltd | Not yet recruiting --> Recruiting
    Enrollment open
    |
    PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    NB003
    almost3years
    A Study of NB003 in Patients With Advanced Malignancies (clinicaltrials.gov)
    P1, N=36, Not yet recruiting, Ningbo Newbay Technology Development Co., Ltd
    Clinical • New P1 trial
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    PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    NB003
    4years
    Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors. (PubMed, Sci Transl Med)
    AZD3229 has a superior potency and selectivity profile to standard of care (SoC) agents-imatinib, sunitinib, and regorafenib, as well as investigational agents, avapritinib (BLU-285) and ripretinib (DCC-2618). AZD3229 has the potential to be a best-in-class inhibitor for clinically relevant KIT/PDGFRα mutations in GIST.
    Journal
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    KDR (Kinase insert domain receptor)
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    KIT mutation
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    imatinib • sunitinib • Stivarga (regorafenib) • Ayvakit (avapritinib) • Qinlock (ripretinib) • NB003