encorafenib + ribociclib

**Encorafenib + ribociclib** is an investigational oral combination therapy consisting of encorafenib, a selective inhibitor of BRAF kinase, and ribociclib, a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. In preclinical models, this combination demonstrated enhanced suppression of tumor growth and prevention or delay of resistance emergence, particularly in BRAF V600E mutant melanoma and experimental models of non-small cell lung cancer. Mechanistically, encorafenib inhibits the MAPK pathway through direct BRAF inhibition, while ribociclib impedes tumor cell proliferation by blocking CDK4/6-mediated phosphorylation of the retinoblastoma (Rb) protein, thereby arresting cell cycle progression in G1. The combination aims to provide synergistic anti-tumor activity and overcome resistance seen with monotherapy. Clinical studies exploring dual and triple combinations with encorafenib, ribociclib, and MEK inhibitor binimetinib have been conducted for BRAF-mutant malignant melanoma and other advanced solid tumors, but encorafenib + ribociclib as a two-drug combination remains investigational and not approved for routine clinical use[1][2][3].

Brand names

KisqaliBraftovi

Other names

ribociclib + encorafenib