Drug intelligence / Profile preview

golvatinib + cetuximab

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

The combination of **golvatinib + cetuximab** is an investigational therapeutic regimen composed of a small molecule tyrosine kinase inhibitor (golvatinib, also known as E7050) and a monoclonal antibody targeting the epidermal growth factor receptor (cetuximab, known as C225 and marketed as Erbitux)[1][3]. **Golvatinib** is an oral dual inhibitor of c-Met and VEGFR (vascular endothelial growth factor receptor) tyrosine kinases, intended to block pathways involved in tumor angiogenesis and proliferation. **Cetuximab** is a chimeric IgG1 monoclonal antibody that binds to EGFR (epidermal growth factor receptor), inhibiting ligand binding, receptor activation, and downstream signaling involved in tumor cell proliferation and survival[1][3]. Combined, the drugs target both the EGFR pathway (cetuximab) and angiogenic/metastatic pathways (golvatinib) to improve tumor control, overcome resistance, and provide a broader anti-tumor effect. This combination has been investigated preclinically for synergistic effects in select solid tumors, particularly those driven by aberrant EGFR and c-Met/VEGF signaling.

Other names
golvatinib + cetuximabE7050 + C225
02

Targets

VEGFR (VEGFR family)EGFR T790M (Epidermal growth factor receptor T790M mutant)MET (Mesenchymal-epithelial transition factor receptor)

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