• Aliases: GDC-0973, XL518
    • An orally bioavailable small-molecule inhibitor of MAP2K1 or MEK1 that specifically binds to and inhibits the catalytic activity of MEK1, resulting in the inhibition of ERK2 phosphorylation and activation and reduced tumor cell proliferation
    • FDA approved for unresectable or metastatic melanoma with BRAF V600E or V600K mutation in combination with vemurafenib
    • Recommended dose: 60 mg daily for 21 days out of the 28-day cycle.
    • Metabolism: Major CYP3A4 substrate
    • Half-life: Average 44 hours (range 23–70 hours)
    • Common side effects: Decreased LVEF, hypertension, photosensitivity, acneiform eruption, hypophosphatemia, increased GGT, nausea/vomiting, ea, anemia, transaminitis, visual impairment, increased SCr
    Other topics in Targeted and Immunotherapy Agents