BEBT-260

BEBT-260 is an orally bioavailable small molecule inhibitor of Extracellular Signal-Regulated Kinase 1 and 2 (ERK1/2), developed by Guangzhou Bibet Pharmaceutical Technology. As the terminal component of the Mitogen-Activated Protein Kinase (MAPK) signaling pathway, ERK1/2 is a critical mediator of cell growth and survival, often hyperactivated in tumors with RAS or BRAF mutations. By inhibiting ERK1/2, BEBT-260 aims to block downstream signaling that promotes cell proliferation and survival, potentially overcoming resistance to upstream MAPK pathway inhibitors such as BRAF and MEK inhibitors. The drug is currently being evaluated in Phase 1 clinical trials for the treatment of patients with advanced solid tumors.