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petosemtamab   Click here for help

GtoPdb Ligand ID: 14238

Synonyms: MCLA-158 | MCLA158
Compound class: Antibody
Comment: Petosemtamab (MCLA-158) is a bispecific epidermal growth factor receptor (EGFR)/leucine-rich repeat-containing G protein-coupled receptor 5 (LGR5) IgG1 monoclonal antibody that was designed for anti-tumour potential [2-3]. In sensitive cancer cells petosemtamab promotes internalisation and degradation of EGFR, inhibits EGFR signalling and engages an anti-tumour immune response via LGR5. It has enhanced ADCC activity against EGFR-driven head and neck squamous cell carcinoma (HNSCC) LGR5-expressing cancer stem cells [1].
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Fayette J, Clatot F, Brana I, Saada E, van Herpen CML, Mazard T, Perez CA, Tabernero J, Le Tourneau C, Hollebecque A et al.. (2024)
Petosemtamab (MCLA-158) with pembrolizumab as first-line (1L) treatment of recurrent/metastatic (r/m) head and neck squamous cell carcinoma (HNSCC): Phase 2 study.
Journal of Clinical Oncology, 42 (16 suppl). DOI: 10.1200/JCO.2024.42.16_suppl.6014
2. Herpers B, Eppink B, James MI, Cortina C, Cañellas-Socias A, Boj SF, Hernando-Momblona X, Glodzik D, Roovers RC, van de Wetering M et al.. (2022)
Functional patient-derived organoid screenings identify MCLA-158 as a therapeutic EGFR × LGR5 bispecific antibody with efficacy in epithelial tumors.
Nat Cancer, 3 (4): 418-436. [PMID:35469014]
3. Lundberg AS, Geuijen CAW, Hill S, Lammerts van Bueren JJ, Fumagalli A, de Kruif J, Silverman PB, Tabernero J. (2025)
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.
Cancers (Basel), 17 (10). [PMID:40427162]
4. Machiels JP, Fayette J, Haddad R, Adkins D, Gillison M, Harrington KJ, Kim SB, Le Tourneau C, Psyrri A, Rosenberg A et al.. (2025)
LiGeR-HN phase III trials of petosemtamab + pembrolizumab and petosemtamab monotherapy in recurrent or metastatic HNSCC.
Future Oncol, 21 (16): 2007-2016. [PMID:40511820]