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    DRUG CLASS:

    EGFR C797S inhibitor

    Related drugs:
    2ms
    A Study to Evaluate the Effect of Food and a Proton Pump Inhibitor on the Pharmacokinetics of VRN110755 (clinicaltrials.gov)
    P1, N=24, Recruiting, Voronoi, Inc | Not yet recruiting --> Recruiting
    Enrollment open
    |
    VRN11
    3ms
    A Study of HS-10504 in Patients With Advanced or Metastatic Non-Small-Cell Lung Cancer(NSCLC) (clinicaltrials.gov)
    P1, N=230, Recruiting, Jiangsu Hansoh Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    3ms
    A Study to Evaluate the Effect of Food and a Proton Pump Inhibitor on the Pharmacokinetics of VRN110755 (clinicaltrials.gov)
    P1, N=24, Not yet recruiting, Voronoi, Inc
    New P1 trial
    |
    VRN11
    6ms
    HS-10375, a selective EGFR C797S tyrosine kinase inhibitor, in advanced non-small cell lung cancer. (PubMed, J Transl Med)
    HS-10375 demonstrated potent and mutant-selective activity against the EGFR C797S mutation in preclinical results, and showed an acceptable safety profile and objective response in a first-in-human phase 1 trial. Trial registration This trial is registered on China Drug Trials (CTR20220045), and ClinicalTrials.gov (NCT05435248).
    Journal • IO biomarker
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    gefitinib • Ameile (aumolertinib) • HS-10375
    7ms
    A Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of AST2303 Tablets (ABK3376 Tablets) in Patients With Advanced or Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=120, Recruiting, Allist Pharmaceuticals, Inc.
    New P1 trial
    1year
    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
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 overexpression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
    |
    Herceptin (trastuzumab) • ER121
    over1year
    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
    |
    EGFR (Epidermal growth factor receptor)
    |
    TRX-221
    almost2years
    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)
    |
    EGFR mutation
    |
    TRX-221
    over2years
    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
    |
    EGFR mutation • EGFR L858R • EGFR T790M • EGFR wild-type • EGFR overexpression • EGFR C797S
    |
    Tagrisso (osimertinib) • TRX-221