Drug intelligence / Profile preview

cetuximab + encorafenib

Development stage
Unknown
Lead developer
Pfizer
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

Cetuximab + encorafenib is a combination regimen of two targeted cancer therapies used primarily for the treatment of metastatic colorectal cancer (mCRC) with a BRAF V600E mutation. Encorafenib is an oral small molecule inhibitor of the BRAF kinase, specifically targeting mutated forms such as BRAF V600E, which drive tumor cell growth through constitutive activation of the MAPK pathway. Cetuximab is an intravenous monoclonal antibody that targets and inhibits the epidermal growth factor receptor (EGFR), blocking downstream signaling involved in cell proliferation and survival. The combination overcomes resistance mechanisms seen with single-agent BRAF inhibition by simultaneously blocking EGFR-mediated feedback activation of MAPK signaling. This regimen has received FDA approval for use after prior therapy in adults with mCRC harboring a BRAF V600E mutation, and more recently under accelerated approval in combination with chemotherapy (mFOLFOX6) for first-line treatment in this population[1][2][3][5][8].

Brand names
BraftoviErbitux
Other names
cetuximab and encorafenibBRAFTOVI plus ERBITUX
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))

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