encorafenib + binimetinib + osimertinib

Encorafenib + binimetinib + osimertinib is an investigational triple-targeted combination regimen consisting of the BRAF inhibitor encorafenib, the MEK inhibitor binimetinib, and the third-generation EGFR tyrosine kinase inhibitor osimertinib. This combination is designed to address a specific resistance mechanism in patients with epidermal growth factor receptor (EGFR)-mutant metastatic non-small cell lung cancer (NSCLC). Approximately 3% of patients with EGFR-mutant NSCLC who progress on osimertinib acquire BRAF alterations (such as BRAF V600E) as an off-target resistance mechanism that reactivates the MAPK signaling pathway. By combining osimertinib with the BRAF/MEK inhibitor pair encorafenib and binimetinib, the regimen aims to simultaneously block both the EGFR and MAPK pathways, thereby overcoming resistance and restoring tumor control. Clinical experience with this triplet regimen is limited, with data primarily derived from a single-center study at the Princess Margaret Cancer Centre.

Other names

Braftovi + Mektovi + TagrissoE+B+OE+B+O regimenencorafenib plus binimetinib plus osimertinibencorafenib, binimetinib, and osimertinib