Encorafenib
Overview + Rationale
- B-Raf is a member of the Raf kinase family of growth signal transduction protein kinases. This protein plays a role in regulating the MAP kinase/ERKs signaling pathway, which affects cell division, differentiation, and secretion
- Activating mutations in BRAF lead to constitutive activation of BRAF and hence RAF-MEK-ERK signaling cascade, promoting cell proliferation and survival while inhibiting apoptosis, and thus driving cancer growth
- Mutations in this gene, most commonly the V600E mutation, are the most frequently identified driver mutations in melanoma
- BRAF mutations have also been identified in various other cancers including colorectal cancer, thyroid carcinoma, non-small cell lung cancer, and hairy cell leukemia
Mechanism of Action
Stage of Development
Encorafenib is being investigated in combination with other agent(s) in the tumor types shown here. Safety and efficacy of encorafenib for the uses listed below has not been established.
BRAF V600E-mutant + Metastatic Colorectal Cancer (mCRC)
Phase 3 Combination* (First Line)
BRAF V600E-mutant and MSI-H Metastatic Colorectal Cancer (mCRC)
Phase 2 Combination (First Line)
BRAF V600E/K-mutant+ Metastatic or Unresectable Locally Advanced Melanoma
Phase 3 (1L) Combination*