First-in-Class Glycosylation Inhibitors for the Treatment of Cancer
Background: Cancer patients with receptor tyrosine kinase (RTK) activating mutations benefit from RTKtargeted therapies, but frequently develop resistance to treatment. Researchers at Yale have pioneered glycosylation inhibitors that block RTK signaling.
Indications: Tumors driven by RTK mutations, including non-small cell lung cancer, colon cancer, head and neck cancer, and breast cancer. Possibly additional indications.
Innovation: Novel small molecule inhibitors of oligosaccharyltransferases (OST) with IC50’s below 100 nM.
Innovator: Joseph N. Contessa, MD, PhD
Patents: US10765638B2; WO2017019540A2