Drug intelligence / Profile preview

petosemtamab + pembrolizumab

Development stage
Unknown
Lead developer
Merus
Modality
Bispecific Antibodies → Multispecific Antibodies → Engineered Antibody Formats → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Petosemtamab + pembrolizumab is an investigational combination therapy comprising petosemtamab (MCLA-158) and pembrolizumab (Keytruda) used in the first-line treatment of recurrent or metastatic head and neck squamous cell carcinoma (HNSCC), specifically in PD-L1–positive patients. Petosemtamab is a bispecific monoclonal antibody targeting both LGR5 and epidermal growth factor receptor (EGFR); it blocks EGF ligand binding, facilitates EGFR internalization and degradation in LGR5+ cells, and induces antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) via enhanced Fc receptor binding. Pembrolizumab is a monoclonal antibody that blocks programmed cell death protein 1 (PD-1), activating the immune system to target tumor cells. The combination is under investigation for superior efficacy compared to pembrolizumab alone, based on encouraging response rates and safety in early clinical studies.

Other names
petosemtamab + pembrolizumab
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)LGR5 (Leucine-rich repeat-containing G-protein coupled receptor 5)PDCD1 (Programmed cell death protein 1 receptor)

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