Drug intelligence / Profile preview

dabrafenib + vemurafenib

Development stage
Discontinued
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Dabrafenib and vemurafenib are both small molecule inhibitors targeting the BRAF kinase, specifically the BRAF V600E mutation. Both drugs are approved as monotherapies for unresectable or metastatic melanoma with a BRAF V600E mutation. However, they are not used together in clinical practice or trials due to overlapping mechanisms and toxicity profiles. Instead, each is typically combined with a MEK inhibitor (dabrafenib with trametinib; vemurafenib with cobimetinib) to improve efficacy and reduce resistance seen with monotherapy. There is no evidence supporting the use of dabrafenib plus vemurafenib as a combination regimen in any indication[1][2][3]. Both drugs act by inhibiting aberrant MAPK pathway signaling driven by mutant BRAF.

02

Targets

RIPK4BRAF V600E

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