petosemtamab

Petosemtamab (MCLA-158) is an investigational bispecific monoclonal antibody developed for the treatment of recurrent or metastatic head and neck squamous cell carcinoma (HNSCC). It targets two proteins commonly expressed on cancer cells—epidermal growth factor receptor (EGFR) and leucine-rich repeat containing G-protein-coupled receptor 5 (LGR5). Petosemtamab exerts its antitumor effects through three independent mechanisms of action: - Inhibition of EGFR-dependent signaling - Binding to LGR5, which leads to internalization and degradation of EGFR in tumor cells and cancer stem cells - Enhancement of antibody-dependent cell-mediated cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP) The drug has received FDA Breakthrough Therapy designation for use as monotherapy in patients with HNSCC who have progressed after platinum-based chemotherapy and anti–PD-1/PD-L1 therapy, as well as in combination with pembrolizumab for first-line treatment in PD-L1–positive HNSCC. Petosemtamab is being developed by Merus.

Other names

PetosemtamabEGFR x LGR5 BiclonicsLgr5 x EGFR BiclonicsLgr-5 x EGFR BiclonicsLgr 5 x EGFR Biclonics