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    DRUG CLASS:

    EGFR degrader

    Related drugs:
    14d
    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
    28d
    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
    2ms
    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
    2ms
    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
    3ms
    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
    11ms
    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
    almost2years
    EGFR degraders in non-small-cell lung cancer: Breakthrough and unresolved issue. (PubMed, Chem Biol Drug Des)
    Osimertinib has become the first globally accessible third-generation EGFR inhibitor, representing one of the most advanced developments in non-small-cell lung cancer (NSCLC) therapy...These degraders compared with EGFR inhibitors showed better efficiency in their cellular potency, inhibition, and toxicity profiles. In this review, we first introduce the structural properties of EGFR, the resistance, and mutations of EGFR, and then mainly focus on the recent advances of EGFR-targeting degraders along with its advantages and outstanding challenges.
    Review • Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR C797S
    |
    Tagrisso (osimertinib)
    2years
    Targeting EGFR degradation by autophagosome degraders. (PubMed, Eur J Med Chem)
    Compound 12c also exhibited promising inhibitory activity, as well as degradation efficiency in vivo. Our study highlights that EGFR-ATTECs could be developed as a new expandable EGFR degradation tool and also reveals a novel potential therapeutic strategy to prevent drug resistance acquired EGFR mutations.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • MAP1LC3B (Microtubule Associated Protein 1 Light Chain 3 Beta)
    |
    EGFR mutation
    over2years
    Ganoderma microsporum immunomodulatory protein as an extracellular epidermal growth factor receptor (EGFR) degrader for suppressing EGFR-positive lung cancer cells. (PubMed, Cancer Lett)
    Our results reveal the interaction mechanisms through which GMI induces EGFR degradation and abolishes EGFR-mediated intracellular pathway. Our study indicates that GMI is an EGFR degrader for inhibiting EGFR-expressing tumor growth.
    Journal • Immunomodulating
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR positive