by LD Rothermel 2024Background: BRAF inhibitors, such as vemurafenib and dabrafenib, are effective in treating patients with melanoma harboring (V600E) BRAF
Profile Name, BRAF V600E/K ; Gene Variant Detail. BRAF V600E/K (gain of function) ; Relevant Treatment Approaches, BRAF Inhibitor MEK inhibitor (Pan) MEK1
BRAF/MEK inhibitor. 1:58
In our studies, we modeled the emergence of resistance to BRAF inhibitors by selecting a panel of BRAFV600E/PTEN melanoma cells which are highly sensitive to BRAF inhibition and chronically exposing them to increasing doses of SB- (GlaxoSmithKline), a BRAF-selective inhibitor . Drug-resistant cells emerged approximately 6 months after
Both immune checkpoint inhibitors (ICI) and molecularly targeted therapy with BRAF and MEK inhibitors (BRAF/MEKi) are standard options for
The BRAF inhibitor dabrafenib and the MEK inhibitor trametinib were each first approved for single-agent use in 2024. The FDA approved combination use of these drugs for BRAF-mutant metastatic
Acquired resistance to BRAF and MEK inhibitor therapy combination is also of significant concern with these drugs, and resistance mechanism are similar to mechanisms of resistance to BRAF inhibitors alone, except in greater magnitudes or in combinations such as BRAF ultra-amplification [Long et al. 2024a].
BRAF inhibitors. Vemurafenib (Zelboraf), dabrafenib (Tafinlar), and encorafenib (Braftovi) are drugs that target the BRAF protein directly.
Dabrafenib is a kinase inhibitor used in the treatment of patients with unresectable or metastatic melanoma with specific BRAF variants. Dabrafenib can be used as a single agent to treat melanoma with the BRAF V600E variant, or in combination with the MEK inhibitor trametinib to treat melanoma with BRAF V600E or V600K variants. BRAF is an intracellular kinase in the
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