Drug intelligence / Profile preview

braf inhibitors + mek inhibitors

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

Overview

Combination of **BRAF inhibitors** and **MEK inhibitors** is a targeted therapy regimen approved for patients with advanced melanoma harboring BRAFV600 mutations. BRAF inhibitors (such as vemurafenib, dabrafenib, encorafenib) block mutant BRAF kinase activity in the MAPK pathway, resulting in reduced tumor proliferation. MEK inhibitors (such as trametinib, cobimetinib, binimetinib) inhibit MEK downstream in the same pathway, preventing resistance and further suppressing tumor cell growth. Compared to single-agent BRAF inhibitors, combination therapy significantly improves progression-free and overall survival, delays resistance, and reduces certain side effects linked to pathway reactivation[1][2][3][5][6][8].

02

Targets

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

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