• Aliases: R115777, Zarnestra (proposed trade name)
    • An orally bioavailable, nonpeptidomimetic quinolinone that binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction, resulting in the prevention of the activation of RAS oncogenes
    • Although theoretically promising as a new agent, the development of this drug has not proceeded successfully to date.
    • Recommended phase 2 dose: 300 mg PO twice daily
    • Half-life: 16 hours
    • Common side effects: Nausea/vomiting, headache, fatigue, anemia, hypotension, liver enzyme elevation, neutropenia, thrombocytopenia
    (Zujewski et al., 2000)
    Other topics in Targeted and Immunotherapy Agents