• Alias: PF-00299804
    • A second-generation small-molecule RTK inhibitor that irreversibly blocks multiple EGFR family receptors (EGFR, HER2, and HER4)
    • Phase 3 studies in metastatic or locally advanced NSCLC with activating EGFR mutations ongoing
    • Recommended phase 3 dose: 45 mg orally once daily
    • Terminal half-life: 51 hours
    • Metabolism: CYP2D6 substrate
    • Common side effects: Diarrhea, dermatitis acneiform (dry skin), stomatitis, paronychia, liver dysfunction (increased bilirubin, ALT/AST), palmar–plantar erythrodysesthesia
    (Bello et al., 2012; Ramalingam et al., 2012)
    Other topics in Targeted and Immunotherapy Agents