drug_type
RELEVANT_DRUG
intervention_type
Biologic (bispecific monoclonal antibody)
drug_description
Bispecific IgG1 monoclonal antibody (MCLA-158) targeting EGFR and LGR5; inhibits EGFR-driven MAPK/PI3K signaling and uses Fc-mediated cytotoxicity/phagocytosis to deplete LGR5+ tumor stem-like cells.
nci_thesaurus_concept_id
C174952
nci_thesaurus_preferred_term
Petosemtamab
nci_thesaurus_definition
An immunoglobulin G1 (IgG1) bispecific antibody targeting both epidermal growth factor receptor (EGFR; HER1; ErbB1) and leucine-rich repeat-containing G-protein coupled receptor 5 (LGR5), with potential antineoplastic activity. Upon administration, petosemtamab simultaneously targets and binds to both EGFR and LGR5, thereby inhibiting the activation of both EGFR- and LGR5-mediated signaling pathways. This results in the inhibition of tumor cell proliferation. EGFR, a receptor tyrosine kinase (RTK) upregulated and/or mutated in a variety of tumor cell types, plays an important role in tumor cell proliferation. LGR5, a member of the Wnt signaling pathway, is a cancer stem cell (CSC) receptor overexpressed on certain cancer cells; it plays a key role in CSC proliferation and survival.
drug_category
INHIBITORY ANTIBODY
drug_class
Inhibitor
drug_delivery_route
Intravenous
drug_mechanism_of_action
Bispecific IgG1 monoclonal antibody that binds EGFR and LGR5 to block EGFR-driven MAPK/PI3K and LGR5/Wnt signaling, inhibiting tumor proliferation; its Fc domain mediates ADCC/ADCP to deplete LGR5+ cancer stem–like cells.
drug_name
Petosemtamab
nct_id_drug_ref
NCT06525220