Epidermal Growth Factor Receptor (EGFR) has emerged as a promising molecular target for the treatment of HNSCC. EGRF is upregulated in most HNSCC tumors notably in advanced stage, large-sized, invasive tumors. These tumors are associated with decreased survival rates and poor prognosis. A variety of therapeutic approaches have been developed to block the upregulation of EGFR, including monoclonal antibody therapies and tyrosine kinase inhibitors, both of which have relatively low clinical responses.

Investigators have developed a class of EGFR antisense agents (EGFRAS) which contain a peptide backbone, called guanidinium peptide nucleic acids (GPNA). These EGFRASGPNAs are believed to bind to the transcriptional start site of the EGFR gene to induce potent and sequence-specific antisense effects while having low toxicity and high specificity.

Stage of Development

• EGFRAS GPNA has shown specific antitumor effects in HNSCC xenografts.

Background
Head and Neck cancers refer to biologically similar cancers originating from the lip, mouth, nose, paranasal sinuses, salivary glands, neck lymph nodes, pharynx, and larynx. Most head and neck cancers are Squamous Cell Carcinomas (SCCHN), originating from the mucosal lining of these regions. HNSCC affects approximately 650,000 patients worldwide and approximately 46,000 new cases are diagnosed in the US every year.

It is an aggressive malignancy where conventional therapeutic interventions like surgery, radio- and chemotherapy have not been promising in improving the five-year survival rates of HNSCC patients. Despite the multidisciplinary treatments, the overall survival rate for advanced cases has not improved for the past 30 years. Furthermore, many of the treatment modalities used for head and neck cancer often result in severe functional and cosmetic deficits. Therefore, the development of novel therapeutic alternatives to standard therapy is needed.

File Number: 1208