Glyco-optimized second-generation cetuximab (Erbitux®)
CetuGEX® is a novel best-in-class immune-enhanced monoclonal antibody (mAb) against the epidermal growth factor receptor (EGFR) with optimized and fully human glycosylation. CetuGEX® works via several anti-tumor mechanisms of action: a strong antibody dependent cellular toxicity (ADCC), proliferation inhibition via receptor blockage and induction of apoptosis.
Disease awareness, and the opportunity
CetuGEX® is a novel best-in-class immune-enhanced monoclonal antibody (mAb) against epidermal growth factor receptor (EGFR) with optimized and fully human glycosylation. There is increasing body of evidence that CetuGEX® may improve the clinical benefit of cancer patients indicated to receive EGFR-targeted therapy. Target indications for clinical development include squamous cell carcinoma of the head and neck (SCCHN), KRAS wild-type-expressing and KRAS mutated colorectal cancer (CRC) as well as non-small cell lung cancer (NSCLC).
In a Phase I dose escalation study, single agent CetuGEX® was well tolerated and showed promising therapeutic activity in patients with various solid tumors, including complete and partial responses and long lasting disease control. In April 2014, Glycotope initiated a Phase 2b study with CetuGEX® to treat squamous cell carcinomas of the head and neck (SCCHN). The recruitment phase for this study has recently been completed. Clinical proof of concept results are expected for mid-2017.
Differentiation/mode of actions/specificity
Due to the optimization of a series of sugar determinants, CetuGEX® has shown to be up to 250-fold more active in anti-tumor ADCC compared to cetuximab, in pre-clinical studies, making CetuGEX® highly potent for patients of all ADCC receptor allotypes and KRAS-mutant patients. This enhanced potency may increase the number of patients and indications suitable for CetuGEX®.