• Alias: BMS-354825
    • Multityrosine kinase inhibitor that was specifically designed to inhibit SRC, which acts as a signal transducer in several molecular pathways within the cell, but was also found to inhibit BCR-ABL and imatinib-resistant mutations of BCR-ABL, except the T315I and F317V mutants; also inhibits KIT, EPHA2, and PDGFRβ
    • FDA approved for chronic or accelerated myeloid leukemia and Ph+ acute lymphoblastic leukemia
    • Recommended dose: 100 to 140 mg orally once daily (preferably with food)
    • Terminal half-life: 3 to 5 hours
    • Metabolism: Major CYP3A4 substrate
    • Common side effects: Myelosuppression, fluid retention leural effusion), nausea/vomiting, diarrhea, headache, musculoskeletal pain, rash, fatigue
    Other topics in Targeted and Immunotherapy Agents