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    DRUG CLASS:

    EGFR C797S inhibitor

    Related drugs:
    11d
    Targeting erbB Pathways in Breast Cancer: Dual Kinase Inhibition for Brain Metastasis and Prevention of p185HER2/Neu Tumor Development. (PubMed, Breast Cancer (Dove Med Press))
    The Herceptin-resistant breast cancer cell line JIMT-1 was used in an in vivo tumor model, and MMTV-erbB2 (Fo5) transgenic mice models were used to evaluate the efficacy and safety of ER121 as neoadjuvant. ER121 is a non-toxic small-molecule erbB kinase inhibitor and holds promise as an oral and systemic therapeutic agent for treating progressive erbB-driven tumors in therapeutic settings. Moreover, ER121 shows potential as a preventive therapy in neoadjuvant settings for erbB2-associated tumors and when administered systemically can dramatically limit erbB2 brain metastases in animal models.
    Journal
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    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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    EGFR mutation • HER-2 overexpression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
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    Herceptin (trastuzumab) • ER121
    5ms
    A Study to Investigate Safety, Tolerability, PK and Anti-tumor Activity of TRX-221 in EGFRm NSCLC Patients (clinicaltrials.gov)
    P1/2, N=115, Recruiting, Therapex Co., Ltd | Not yet recruiting --> Recruiting
    Enrollment open
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    EGFR (Epidermal growth factor receptor)
    |
    TRX-221
    11ms
    A Study to Investigate Safety, Tolerability, PK and Anti-tumor Activity of TRX-221 in EGFRm NSCLC Patients (clinicaltrials.gov)
    P1/2, N=115, Not yet recruiting, Therapex Co., Ltd
    New P1/2 trial
    |
    EGFR (Epidermal growth factor receptor)
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    EGFR mutation
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    TRX-221
    over1year
    TRX-221, a novel 4th-generation EGFR inhibitor for overcoming C797S mutation-mediated acquired resistance in NSCLC (AACR 2023)
    With favorable DMPK profiles, once-daily oral dosing of TRX-221 induced strong anti-tumor effects in a dose-dependent manner in a variety of osimertinib-resistant CDX and PDX models. As a reversible, selective, and broad-spectrum 4th-generation EGFR-TKI, TRX-221 is currently undergoing IND-enabling studies and shows strong potential as a therapeutic solution to treat advanced NSCLC patients harboring EGFR mutations.
    Preclinical
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    EGFR mutation • EGFR L858R • EGFR T790M • EGFR wild-type • EGFR overexpression • EGFR C797S
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    Tagrisso (osimertinib) • TRX-221