Drug intelligence / Profile preview

encorafenib + binimetinib

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Encorafenib and binimetinib are small-molecule, oral targeted cancer therapies used in combination to treat adults with unresectable or metastatic melanoma and metastatic non-small cell lung cancer (NSCLC) harboring a BRAF V600 mutation. Encorafenib is a selective inhibitor of mutant BRAF kinases (including V600E, V600D, and V600K), while binimetinib is a reversible inhibitor of MEK1 and MEK2. Both drugs act on the MAP kinase/ERK signaling pathway, which regulates cell proliferation. By inhibiting both BRAF and MEK kinases, this combination blocks ERK phosphorylation more effectively than either agent alone—resulting in decreased tumor cell growth, delayed resistance development, and reduced toxicity compared to monotherapy. The combination is indicated for patients whose tumors have tested positive for the BRAF V600 mutation[1][3][5][6].

Brand names
BraftoviMektovi
Other names
encorafenib + binimetinib
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)CAPN3 (B-Raf proto-oncogene, serine/threonine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)RAF1 (c-Raf-1 (Y340D/Y341D))MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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