Leukemias, lymphomas, and other hematologic cancers:
Indications for: BOSULIF
Newly-diagnosed chronic phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy.
Take with food. Swallow whole. Continue until disease progression or patient intolerance. Newly-diagnosed: 400mg once daily. Renal impairment (CrCl 30–50mL/min): initially 300mg daily; (CrCl <30mL/min): initially 200mg daily. With resistance/intolerance to prior therapy: 500mg once daily. Renal impairment (CrCl 30–50mL/min): initially 400mg daily; (CrCl <30mL/min): initially 300mg daily. Both: hepatic impairment: initially 200mg daily. Dose escalation or dose adjustments for toxicity: see full labeling.
<18yrs: not established.
Monitor and manage GI toxicity, cardiac failure/ischemia, fluid retention; withhold, reduce dose, or discontinue as necessary. Coronary artery disease risk factors (including history of diabetes, BMI >30, hypertension, vascular disorders): higher occurrence of cardiac ischemic events. Perform CBC weekly for first month, then monthly; hepatic enzyme tests monthly for first 3 months (more frequently if transaminase elevations occur); withhold, reduce dose, or discontinue as necessary. Monitor renal function at baseline and during therapy; consider adjusting dose if renal impairment occurs. Dialysis: not studied. Embryo-fetal toxicity. Pregnancy: exclude status prior to initiation. Advise females of reproductive potential to use effective contraception during and for ≥2 weeks after the last dose. Nursing mothers: not recommended (during and for ≥2 weeks after the last dose).
Tyrosine kinase inhibitor.
Potentiated by strong or moderate CYP3A inhibitors (eg, ketoconazole, aprepitant, grapefruit products); avoid concomitant use. Antagonized by strong CYP3A inducers (eg, rifampin, St. John’s wort); avoid concomitant use. Antagonized by proton pump inhibitors (eg, lansoprazole); consider short-acting antacids or H2 blockers instead; separate dosing by >2hrs.
Diarrhea, rash, nausea, abdominal pain, vomiting, fatigue, hepatic dysfunction, respiratory tract infection, pyrexia, headache, lab abnormalities; myelosuppression, pneumonia, pleural effusion, coronary artery disease, gastroenteritis.
Fecal (91.3%), renal (3.3%).
Mean half-life (SD): 22.5 (1.7) hours. Mean clearance (SD): 189 (48) L/h.
Generic Drug Availability:
Tabs 100mg—120; 400mg, 500mg—30