GateKeeper

Gatekeeper Pharmaceuticals was a biotechnology company founded in 2009 by researchers from the Dana-Farber Cancer Institute to develop next-generation small molecule inhibitors for non-small cell lung cancer (NSCLC). The company’s research focused on overcoming resistance to first-generation EGFR inhibitors by targeting the T790M "gatekeeper" mutation. Its lead compound, WZ-4-002, was a first-in-class third-generation EGFR tyrosine kinase inhibitor (TKI) that demonstrated high selectivity for the T790M mutation over wild-type EGFR. However, the company’s development efforts were derailed by a protracted legal battle with Novartis and Dana-Farber over intellectual property rights, which eventually led to the company becoming inactive. The underlying technology was subsequently licensed to Clovis Oncology, contributing to the development of the clinical-stage inhibitor rociletinib.