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    DRUG:

    limertinib (ASK120067)

    i
    Other names: ASK120067, ASK-120067
    Company:
    Aosaikang Pharma, Innovent Biologics
    Drug class:
    EGFR inhibitor
    Related drugs:
    12d
    Neoadjuvant Sacituzumab Tirumotecan and Limertinib for Potentially Resectable Stage Ⅲ EGFR-mutant Non-small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=36, Recruiting, Shanghai Pulmonary Hospital, Shanghai, China
    New P2 trial
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation
    |
    Jiataile (sacituzumab tirumotecan) • limertinib (ASK120067)
    28d
    ASKC202-001: Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Anti-tumor Activity of ASKC202 With or Without ASK120067 (clinicaltrials.gov)
    P1, N=150, Recruiting, Jiangsu Aosaikang Pharmaceutical Co., Ltd. | Trial completion date: May 2025 --> Dec 2027 | Trial primary completion date: May 2024 --> Dec 2026
    Trial completion date • Trial primary completion date
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET amplification
    |
    limertinib (ASK120067) • ASKC202
    3ms
    ​Efficacy and Safety of Limertinib Combined with Radioactive Iodine-125 Seed Implantation in Patients with EGFR-Mutant Advanced Non-Squamous Non-Small Cell Lung Cancer Exhibiting Oligoprogression After Prior EGFR-TKI Therapy: A Prospective, Single-Arm, Multicenter, Observational Study​ (ChiCTR2500110139)
    P4, N=33, Not yet recruiting, Hebei General Hospital​; Hebei General Hospital
    New P4 trial
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    limertinib (ASK120067)
    6ms
    ASKC202 Combined With Limertinib Versus Platinum-based Chemotherapy in Treatment of Locally Advanced or Metastatic NSCLC With MET Amplification/Overexpression After Failure of EGFR-TKI Therapy (clinicaltrials.gov)
    P3, N=286, Not yet recruiting, Jiangsu Aosaikang Pharmaceutical Co., Ltd.
    New P3 trial
    |
    cisplatin • carboplatin • pemetrexed • limertinib (ASK120067) • ASKC202
    6ms
    A Multicenter Phase II Randomized Trial of Limertinib Followed by Sintilimab and Chemotherapy vs. Limertinib Followed by Limertinib and Chemotherapy as Neoadjuvant Therapy in Resectable Stage II–IIIB EGFR-Mutant NSCLC (ChiCTR2500106897)
    P2, N=134, Not yet recruiting, Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sciences); Guangdong Provincial People's Hospital(Guangdong Academy of Medical Sci
    New P2 trial
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1)
    |
    EGFR mutation
    |
    cisplatin • carboplatin • Tyvyt (sintilimab) • pemetrexed • limertinib (ASK120067)
    7ms
    Efficacy and safety of limertinib versus gefitinib as first-line treatment for locally advanced or metastatic non-small-cell lung cancer with EGFR-sensitising mutation: a randomised, double-blind, double-dummy, phase 3 trial. (PubMed, Lancet Respir Med)
    Limertinib showed superior efficacy compared with gefitinib and a manageable safety profile for locally advanced or metastatic NSCLC patients with EGFR-sensitising mutation and should be considered as another first-line treatment option for this patient population.
    P3 data • Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    cobas® EGFR Mutation Test v2
    |
    gefitinib • limertinib (ASK120067)
    8ms
    A prospective, controlled Phase II clinical study on the efficacy and safety of the combination of lerotinib and bevacizumab versus lerotinib monotherapy as first - line treatment for locally advanced or recurrent metastatic non - squamous NSCLC with EGFR mutations and high PD-L1 expression. (ChiCTR2500101370)
    P2, N=136, Not yet recruiting, Shanghai Chest Hospital; Shanghai Chest?Hospital
    New P2 trial • IO biomarker
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression • EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    Avastin (bevacizumab) • limertinib (ASK120067)
    8ms
    LIBRA: A Clinical Study on the Efficacy and Safety of the Combination of Limertinib and Bevacizumab Versus Limertinib as First-line Treatment for NSCLC. (clinicaltrials.gov)
    P2, N=136, Not yet recruiting, Shanghai Chest Hospital
    New P2 trial • IO biomarker
    |
    PD-L1 (Programmed death ligand 1)
    |
    Avastin (bevacizumab) • limertinib (ASK120067)
    over1year
    Branched-chain amino acid transaminase 1 confers EGFR-TKI resistance through epigenetic glycolytic activation. (PubMed, Signal Transduct Target Ther)
    In this study, we conducted a comprehensive investigation utilizing high-throughput proteomics analysis on established TKI-resistant tumor models, and found a notable upregulation of branched-chain amino acid transaminase 1 (BCAT1) expression in both osimertinib- and ASK120067-resistant tumors compared with the parental TKI-sensitive NSCLC tumors. Moreover, we identified WQQ-345 as a novel BCAT1 inhibitor exhibiting antitumor activity both in vitro and in vivo against TKI-resistant lung cancer with high BCAT1 expression. In summary, our study highlighted the crucial role of BCAT1 in mediating resistance to third-generation EGFR-TKIs through epigenetic activation of glycolysis in NSCLC, thereby supporting BCAT1 as a promising therapeutic target for the treatment of TKI-resistant NSCLC.
    Journal
    |
    BCAT1 (Branched Chain Amino Acid Transaminase 1 )
    |
    Tagrisso (osimertinib) • limertinib (ASK120067)
    over1year
    ASK120067 Versus Gefitinib as First-line Treatment for EGFRm Locally Advanced or Metastatic NSCLC (clinicaltrials.gov)
    P3, N=337, Active, not recruiting, Jiangsu Aosaikang Pharmaceutical Co., Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Dec 2023 --> Sep 2026 | Trial primary completion date: Mar 2023 --> Mar 2024
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    gefitinib • limertinib (ASK120067)
    over1year
    AM-DMF-SCP: Integrated Single-Cell Proteomics Analysis on an Active Matrix Digital Microfluidic Chip. (PubMed, JACS Au)
    Applying the AM-DMF-SCP to characterize the proteomes of a third-generation EGFR inhibitor, ASK120067-resistant cells (67R) and their parental NCI-H1975 cells, we observed a potential correlation between elevated VIM expression and 67R resistance, which is consistent with the findings from bulk sample analyses. These results suggest that AM-DMF-SCP is an automated, robust, and sensitive platform for single-cell proteomics and demonstrate the potential for providing valuable insights into cellular mechanisms.
    Journal
    |
    VIM (Vimentin)
    |
    limertinib (ASK120067)