BRAF Inhibitor
Overview + Rationale
Overview
- B-Raf is a member of the Raf kinase family of growth signal transductionprotein kinases. This protein plays a role in regulating the MAP kinase/ERKssignaling pathway, which affects cell division, differentiation, and secretion
- Activating mutations in BRAF lead to constitutive activation of BRAF and henceRAF-MEK-ERK signaling cascade, promoting cell proliferation and survival whileinhibiting apoptosis, and thus driving cancer growth
- Mutations in this gene, most commonly the V600E mutation, are the mostfrequently identified driver mutations in melanoma
- BRAF mutations have also been identified in various other cancers includingcolorectal cancer, thyroid carcinoma, non-small cell lung cancer, and hairy cellleukemia
Stage of Development
BRAF V600E-mutant+Metastatic ColorectalCancer (mCRC)
Phase 3 Combination(First Line)