• Alias: LGX818
    • Specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/MEK/ERK signaling pathway
    • Phase 3 study in mCRC with encorafenib, binimetinib, and cetuximab with mutated BRAF; phase 3 study of encorafenib plus binimetinib versus encorafenib in BRAF mutant melanoma
    • Half-life: â™30 hours
    • Recommended phase 2 dose: 200 to 400 mg PO daily
    • Common side effects: Anemia, hyperglycemia, increased lipase, hypertension, fatigue, nausea, arthralgia, palmar–plantar erythrodysesthesia
    (Dummer et al., 2017)
    Other topics in Targeted and Immunotherapy Agents