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    DRUG CLASS:

    EGFR degrader

    Related drugs:
    14d
    Overcoming Cetuximab Resistance in HNSCC by Hsp90 Inhibition to Enhance EGFR Degradation. (PubMed, J Biol Chem)
    Histopathological analysis confirmed that therapeutic efficacy was driven by a significant reduction in EGFR protein levels. Our findings establish Hsp90-mediated stabilization of monomeric EGFR as a novel resistance mechanism and provide a translational rationale for employing low-dose Hsp90 inhibition in combination with cetuximab to improve clinical outcomes for HNSCC patients currently lacking effective targeted options.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • HSP90AA1 (Heat Shock Protein 90 Alpha Family Class A Member 1Heat Shock Protein 90 Alpha Family Class A Member 1)
    |
    KRAS mutation • EGFR expression
    |
    Erbitux (cetuximab)
    2ms
    BG-60366-101: A Study Investigating BG-60366 in Adults With Epidermal Growth Factor Receptor (EGFR)-Mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=33, Terminated, BeOne Medicines | Active, not recruiting --> Terminated; Evaluation on business strategy, not involving safety issue.
    Trial termination
    |
    EGFR mutation
    3ms
    BG-60366-101: A Study Investigating BG-60366 in Adults With Epidermal Growth Factor Receptor (EGFR)-Mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=33, Active, not recruiting, BeOne Medicines | N=93 --> 33 | Trial completion date: Apr 2028 --> May 2026 | Trial primary completion date: Apr 2028 --> May 2026 | Recruiting --> Active, not recruiting
    Enrollment closed • Enrollment change • Trial completion date • Trial primary completion date
    |
    EGFR mutation
    3ms
    A Phase 1 Study of EPI-326 in EGFR-mutant NSCLC and HNSCC (clinicaltrials.gov)
    P1, N=110, Recruiting, EpiBiologics | Not yet recruiting --> Recruiting
    Enrollment open • First-in-human
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    4ms
    A Phase 1 Study of EPI-326 in EGFR-mutant NSCLC and HNSCC (clinicaltrials.gov)
    P1, N=110, Not yet recruiting, EpiBiologics
    New P1 trial • First-in-human
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    5ms
    A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics, and Preliminary Anti-tumor Efficacy of HJ-004-02 Tablets in Patients with Advanced Non-squamous Non-small Cell Lung Cancer with Epidermal Growth Factor Receptor (EGFR) Mutations (ChiCTR2500112428)
    P1, N=36, Not yet recruiting, Shanghai East Hospital; Jing Medicine Technology (Shanghai) Co., Ltd.
    New P1 trial
    |
    EGFR mutation • EGFR L858R • EGFR T790M • EGFR exon 20 insertion • EGFR expression • EGFR L861Q • EGFR S768I • EGFR positive
    5ms
    A Phase 1a/1b Study Investigating the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Antitumor Activity of BG-60366 in Patients With EGFR-Mutant Non-Small Cell Lung Cancer (ChiCTR2500113951)
    P1, N=258, Not yet recruiting, Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sciences); Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sci
    New P1 trial
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion • EGFR L861Q • EGFR G719X • EGFR S768I
    5ms
    HJ-004-02-101: A Phase l Clinical Study to Evalute the Safety,Tolerability,Pharmacokinetic Characteristics,and Preliminary Anti-tumor Efficacy of HJ-004-02 Tablets in Patients With Non-squamous Non-small Cell Lung Cancer With Epidermal Growth Factor Receptor (EGFR) Mutations (clinicaltrials.gov)
    P1, N=36, Recruiting, Tongji University
    New P1 trial
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR positive
    1year
    Discovery of potent CRBN-recruiting epidermal growth factor receptor (EGFR) degraders in vitro. (PubMed, Invest New Drugs)
    In this paper, we designed and synthesized a series of small molecule PROTACs targeting EGFR utilizing WZ4002, known for its mutation selectivity, as the warhead...Further analysis through protein immunoblotting revealed that HJM- 17 effectively reduced the expression of EGFRL858R/T790M. These active compounds lay the groundwork for future studies focused on EGFR-targeting PROTACs.
    Preclinical • Journal
    |
    EGFR (Epidermal growth factor receptor) • CRBN (Cereblon)
    |
    EGFR mutation • EGFR L858R • EGFR T790M
    |
    WZ4002
    over1year
    BG-60366-101: A Study Investigating BG-60366 in Adults With Epidermal Growth Factor Receptor (EGFR)-Mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=93, Recruiting, BeiGene | Not yet recruiting --> Recruiting
    Enrollment open
    over1year
    Discovery of a molecular glue for EGFR degradation. (PubMed, Oncogene)
    Notably, CDDO-Me attenuates TNBC progression by accelerating EGFR degradation in cell-derived xenografts and patient-derived organoid models, highlighting its clinical application potential. Consequently, induction of EGFR degradation through MG degraders represents a viable therapeutic strategy for TNBC.
    Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR expression
    over1year
    A Study Investigating BG-60366 in Adults With Epidermal Growth Factor Receptor (EGFR)-Mutant Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=93, Not yet recruiting, BeiGene
    New P1 trial