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    DRUG CLASS:

    EGFR antagonist

    Related drugs:
    2ms
    An anti-PD-1 antibody (SCT-I10A) plus anti-EGFR antibody (SCT200) and chemotherapy for RAS/BRAF wild-type metastatic colorectal cancer: A phase Ib study. (PubMed, Cancer Lett)
    Immunotherapy has demonstrated limited efficacy against microsatellite-stable (MSS) metastatic colorectal cancer (mCRC). Oxaliplatin may induce greater immune activation, with GZMA and CXCL13 serving as potential prognostic biomarkers. Thus, combining immunotherapy, EGFR inhibitors, and XELOX represents an optimal therapeutic strategy for mCRC.
    P1 data • Journal • PD(L)-1 Biomarker • IO biomarker
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    BRAF (B-raf proto-oncogene) • CXCL13 (Chemokine (C-X-C motif) ligand 13) • GZMA (Granzyme A)
    |
    BRAF wild-type
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    capecitabine • oxaliplatin • SCT200 • Anyouping (finotonlimab)
    3ms
    Multi-Omics and Single-Cell Insights Reveal a Lysophosphatidic Acid (LPA)-Mediated Resistant Mechanism to Third Generation EGFR-TKI in Non-Small Cell Lung Cancer. (PubMed, Clin Cancer Res)
    Our study highlights the pivotal role of LPA-mediated signaling and metabolic reprogramming in third-generation EGFR-TKI resistance. Targeting LPA production or its downstream pathways may offer novel therapeutic strategies to overcome resistance. This study provides critical metabolic insights for managing EGFR-sensitive-mutant NSCLC.
    Journal
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    TGFB1 (Transforming Growth Factor Beta 1)
    |
    EGFR mutation
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    Rui Bi Da (rezivertinib)
    4ms
    Artificial intelligence combined with affinity chromatography discover that 7-Epitaxol promotes autophagy in NSCLC cells by interacting with EGFR: Discovery of novel EGFR antagonist based on DL and CMC. (PubMed, Phytomedicine)
    The results provide a novel and powerful platform for drug discovery and development in NSCLC research. By using this platform, Geraniin, Brazilin, and 7-epitaxol were identified as novel EGFR antagonists. We also innovatively demonstrated that 7-epitaxol promotes autophagy in NSCLC.
    Journal
    |
    EGFR (Epidermal growth factor receptor)
    6ms
    Petosemtamab, a Bispecific Antibody Targeting Epidermal Growth Factor Receptor (EGFR) and Leucine-Rich G Repeat-Containing Protein-Coupled Receptor (LGR5) Designed for Broad Clinical Applications. (PubMed, Cancers (Basel))
    The safety profile is generally favorable, with low rates of skin and gastrointestinal toxicity. Phase 3 trials are ongoing in both first-line programmed death-ligand 1-positive (PD-L1+) and second/third-line r/m HNSCC.
    Review • Journal
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    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1) • LGR5 (Leucine Rich Repeat Containing G Protein-Coupled Receptor 5)
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    PD-L1 expression
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    petosemtamab (MCLA-158)
    10ms
    Rezivertinib versus gefitinib as first-line therapy for patients with EGFR-mutated locally advanced or metastatic non-small-cell lung cancer (REZOR): a multicentre, double-blind, randomised, phase 3 study. (PubMed, Lancet Respir Med)
    Our findings suggested that rezivertinib is a potential choice for patients with EGFR-mutated locally advanced or metastatic NSCLC as first-line therapy, owing to the superior overall efficacy and subgroup progression-free survival compared with gefitinib in targeted patients. No new safety signals were identified.
    P3 data • Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR exon 19 deletion
    |
    gefitinib • Rui Bi Da (rezivertinib)
    1year
    Spatial analyses revealed S100P + TFF1 + tumor cells in spread through air spaces samples correlated with undesirable therapy response in non-small cell lung cancer. (PubMed, J Transl Med)
    To assess the role of S100P + TFF1 + tumor cells in therapy response, we included data from two clinical trial cohorts (BPI-7711 for EGFR-TKI therapy and ORIENT-3 for immunotherapy)...This was further validated by multiplex immunofluorescence performed on twenty NSCLC samples. In summary, our study identified S100P as the biomarker for STAS and highlighted the adverse role of S100P + TFF1 + tumor cells in survival outcomes.
    Journal • IO biomarker • Tumor cell
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    TGFBR2 (Transforming Growth Factor Beta Receptor 2) • TFF1 (Trefoil Factor 1) • S100P (S100 calcium binding protein P) • TGFB2 (Transforming Growth Factor Beta 2)
    |
    Rui Bi Da (rezivertinib)
    over1year
    Phase I Clinical Trial of CDP1 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=32, Completed, Dragonboat Biopharmaceutical Company Limited | Unknown status --> Completed
    Trial completion • Metastases
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    BRAF (B-raf proto-oncogene) • RAS (Rat Sarcoma Virus)
    |
    cisplatin • paclitaxel • BC001 (cetuximab biosimilar)
    over1year
    MCLA-158-CL03: A Phase 3 Study to Evaluate Petosemtamab Plus Pembrolizumab vs Pembrolizumab in First-line Treatment of Head and Neck Cancer (clinicaltrials.gov)
    P3, N=500, Recruiting, Merus N.V. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    over1year
    A Study of BPI-7711 Capsule in Non-small Cell Lung Cancer Patients (clinicaltrials.gov)
    P3, N=369, Active, not recruiting, Beta Pharma Shanghai | Trial completion date: Feb 2024 --> Dec 2025
    Trial completion date • Metastases
    |
    gefitinib • Rui Bi Da (rezivertinib)
    over1year
    KL140-Ⅲ-02-CTP: Comparison of A140 and Erbitux Combined With mfolfox6 to Evaluate Efficacy and Safety of First-line Treatment for Ras Wild-type mCRC (clinicaltrials.gov)
    P3, N=688, Completed, Sichuan Kelun Pharmaceutical Research Institute Co., Ltd. | Recruiting --> Completed | Trial completion date: Apr 2023 --> Jan 2024
    Trial completion • Trial completion date
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
    |
    Erbitux (cetuximab) • 5-fluorouracil • oxaliplatin • Datalai (cetuximab biosimilar)
    over1year
    A Phase 3 Study to Evaluate Petosemtamab Plus Pembrolizumab vs Pembrolizumab in First-line Treatment of Recurrent or Metastatic PD-L1+ Head and Neck Squamous Cell Carcinoma Patients (clinicaltrials.gov)
    P3, N=500, Not yet recruiting, Merus N.V.
    New P3 trial • Metastases
    |
    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    over1year
    LiGeR-HN2: A Phase 3 Study to Evaluate Petosemtamab Compared With Investigator's Choice Monotherapy in Previously Treated Head and Neck Squamous Cell Carcinoma Patients (clinicaltrials.gov)
    P3, N=500, Recruiting, Merus N.V. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    Erbitux (cetuximab) • docetaxel • petosemtamab (MCLA-158)