• Alias: PS-341
    • Reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquitinated protein with an unusual boron “backbone”
    • Inhibits nuclear factor NFκB, a protein that is constitutively activated in some cancers, thereby interfering with NFκB–mediated cell survival, tumor growth, and angiogenesis
    • FDA approved for MM
    • Recommended dose: 1.3 mg/m2 IV twice weekly for 2 weeks followed by a 10-day rest period. New recommendation for subcutaneous route
    • Half-life: 9 to 15 hours
    • Metabolism: Major substrate of CYP3A4 and CYP2C19
    • Common side effects: Peripheral neuropathy, neutropenia, thrombocytopenia, GI effects, asthenia
    Other topics in Targeted and Immunotherapy Agents