GtoPdb is requesting financial support from commercial users. Please see our sustainability page for more information.

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].
Click here for help
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
LGR5 Hs Antibody Binding 9.2 pKd - 2
pKd 9.2 (Kd 6.6x10-10 M) [2]
Selectivity at catalytic receptors
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
epidermal growth factor receptor Hs Antibody Binding 9.7 pKd - 2
pKd 9.7 (Kd 2.2x10-10 M) [2]