• Aliases: SKI-606
    • BRC-ABL inhibitor with activities against SRC family (including SRC, LYN, and HCK)
    • Very minimal activity in KIT and PDGFR
    • Activity in 16 of 18 imatinib-resistant BCR-ABL mutations, with exceptions being the T315I and V299L mutants
    • FDA approved for Ph+ chronic myelogenous leukemia
    • Recommended dose: 500 mg orally once daily with food
    • Half-life: 22 hours
    • Metabolism: Major CYP3A4 substrate and P-glycoprotein
    • Common side effects: Nausea/vomiting, diarrhea, edema, myelosuppression, rash, abdominal pain, pyrexia, transaminitis
    • Clinical pearls: Do not take proton pump inhibitors while on bosutinib. Short-acting antacids and H2 antagonists may of bosutinib. Take this medicine with food and a glass of water. Do not crush, break, or chew the tablets. The median time to the onset of side effects is typically 2 days.
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