GW5282

GW5282 is an orally bioavailable small molecule inhibitor of General Control Nonderepressible 2 (GCN2) kinase, also known as EIF2AK4, currently under development by Dizal Pharmaceuticals. GCN2 serves as a metabolic sensor that detects amino acid deficiency in the tumor microenvironment, triggering the integrated stress response (ISR) to promote cell survival and immunosuppression. By blocking GCN2 activity, GW5282 is designed to disrupt the adaptive stress response of tumor cells and potentially enhance anti-tumor immune responses by modulating the metabolic state of immune cells. It is being investigated in Phase 1/2 clinical trials for patients with advanced or metastatic solid tumors and hematological malignancies.