BRAF inhibitor
BRAF kinase inhibitor
- Blocks mutant BRAF → shuts down MAPK (mitogen-activated protein kinase) growth signaling
- Suppresses BRAF-V600–driven melanoma and other tumors
- Paradoxical MAPK activation in BRAF-wild-type cells → cutaneous squamous cell carcinomas unless paired with a MEK inhibitor
Drugs with this mechanism (3)
- Dabrafenib — BRAF V600 inhibitor; paradoxically activates the pathway in BRAF-wild-type cells.
- Sorafenib — Multikinase inhibitor for selected liver, kidney, and thyroid cancers; hand-foot skin reaction, diarrhea, and hypertension are prominent.
- Vemurafenib — BRAF inhibitor for BRAF-V600E melanoma.
Self-check
- In which cells can BRAF inhibition paradoxically activate MAPK?
BRAF-wild-type cells. - What paired inhibitor counters the cutaneous squamous-carcinoma risk described here?
A MEK inhibitor.
All mechanisms · Open BRAF inhibitor in the interactive console ↗