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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].
Ligand Activity Visualisation ChartsThese 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. ✖ |
| No information available. |
Summary of Clinical Use  |
| Petosemtamab (MCLA-158) has progressed to late stage clinical development for potential to treat head and neck squamous cell carcinoma (HNSCC). It was garnted FDA Breakthrough Therapy Designation for this indication in early 2025. |
| Clinical Trials | |||||
| Clinical Trial ID | Title | Type | Source | Comment | References |
| NCT03526835 | A Study of Bispecific Antibody MCLA-158 in Patients With Advanced Solid Tumors | Phase 1/Phase 2 Interventional | Merus N.V. | 1 | |
| NCT06496178 | A Phase 3 Study to Evaluate Petosemtamab Compared With Investigator's Choice Monotherapy in Previously Treated Head and Neck Squamous Cell Carcinoma Patients | Phase 3 Interventional | Merus N.V. | 4 | |
| NCT06525220 | A Phase 3 Study to Evaluate Petosemtamab Plus Pembrolizumab vs Pembrolizumab in First-line Treatment of Head and Neck Cancer (LiGeR - HN1) | Phase 3 Interventional | Merus N.V. | 4 | |
