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    DRUG CLASS:

    LGR5 inhibitor

    Related drugs:
    24d
    Immunotherapeutic strategies in HPV-positive and HPV-negative recurrent/metastatic oropharyngeal squamous cell carcinoma: from PD-1 blockade to EGFR-directed bispecifics and therapeutic HPV vaccines. (PubMed, Crit Rev Oncol Hematol)
    Emerging agents such as ficerafusp alfa, petosemtamab, and amivantamab have demonstrated promising early clinical activity, particularly in biomarker-enriched or post-immunotherapy settings. In HPV-positive disease, therapeutic vaccines targeting E6/E7 oncoproteins have shown encouraging immunogenicity and preliminary antitumor activity, especially when combined with PD-1 blockade. Overall, the immunotherapeutic landscape of OPSCC is evolving toward a biomarker-driven framework integrating viral status, immune contexture and pathway activation to enable more precise and personalized treatment strategies.
    Review • Journal • PD(L)-1 Biomarker • IO biomarker
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    EGFR (Epidermal growth factor receptor) • TGFB1 (Transforming Growth Factor Beta 1)
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    ficerafusp alfa (BCA101) • petosemtamab (MCLA-158)
    1m
    MCLA-158-CL04: A Phase 2 Study of Petosemtamab in Combination with Pembrolizumab in Adults with NSCLC (2025-522867-13-00)
    P1/2, N=90, Recruiting, Merus B.V. | N=45 --> 90
    Enrollment change
    |
    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    1m
    MCLA-158-CL04: A Phase 2 Study of Petosemtamab in Combination with Pembrolizumab in Adults with NSCLC (2025-522867-13-00)
    P1/2, N=90, Recruiting, Merus B.V. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    2ms
    LiGeR-HN1: A Phase 3 Study to Evaluate Petosemtamab Plus Pembrolizumab vs Pembrolizumab in First-line Treatment of Head and Neck Cancer (LiGeR - HN1) (clinicaltrials.gov)
    P3, N=700, Recruiting, Merus B.V. | N=500 --> 700
    Enrollment change
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    PD-L1 (Programmed death ligand 1) • CD4 (CD4 Molecule)
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    PD-L1 expression
    |
    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    2ms
    MCLA-158-CL04: A Phase 2 Study of Petosemtamab in Combination with Pembrolizumab in Adults with NSCLC (2025-522867-13-00)
    P1/2, N=45, Not yet recruiting, Merus N.V.
    New P1/2 trial
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    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    2ms
    Study to Investigate Petosemtamab in Adults With Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=180, Recruiting, Merus B.V. | Initiation date: Dec 2025 --> Mar 2025
    Trial initiation date
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    PD-L1 (Programmed death ligand 1)
    |
    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    5ms
    Study to Investigate Petosemtamab in Adults With Metastatic Non-Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=180, Recruiting, Merus N.V.
    New P2 trial
    |
    PD-L1 (Programmed death ligand 1)
    |
    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    1year
    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)
    |
    PD-L1 expression
    |
    petosemtamab (MCLA-158)
    almost2years
    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)
    almost2years
    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
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    Keytruda (pembrolizumab) • petosemtamab (MCLA-158)
    almost2years
    QPH-FR: A Novel Quinoa Peptide Enhances Chemosensitivity by Targeting Leucine-Rich Repeat-Containing G Protein-Coupled Receptor 5 in Colorectal Cancer. (PubMed, J Agric Food Chem)
    Mechanistically, QPH-FR competitively suppressed the formation of the LGR5/RSPO1 complex by binding to LGR5, causing RNF43/ZNRF3 to ubiquitinate the FZD receptor, thereby suppressing the Wnt/β-catenin signaling pathway and exerting stemness inhibition. In summary, the study proposes that a novel peptide QPH-FR from quinoa elucidates the mechanism by which QPH-FR targets LGR5 to enhance chemosensitivity, providing theoretical support for the development of chemotherapeutic adjuvant drugs based on plant peptides.
    Journal
    |
    RNF43 (Ring Finger Protein 43) • RSPO1 (R-Spondin 1) • ZNRF3 (Zinc And Ring Finger 3)
    |
    5-fluorouracil
    almost2years
    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)