• Aliases: MSC1936369B, AS703026
    • A small molecule that selectively binds to and inhibits the activity of MEK1/2
    • Currently under investigation in phase 1/2 clinical trials in NRAS+ cutaneous melanoma (phase 2), pancreatic cancer (phases 1 and 2), and low-grade ovarian cancer (phase 1)
    • Recommended phase 2 dose: 60 mg PO b.i.d. Not to be taken with any proton pump inhibitors or H2 antagonist or antacids because of compromised absorption
    • Terminal half-life: â™5 hours
    • Metabolism: Major CYP3A4 and CYP2C19 substrate
    • Common side effects: Skin rash, diarrhea, ocular events, asthenia, peripheral edema, nausea/vomiting
    Other topics in Targeted and Immunotherapy Agents