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, fluid retention; withhold, reduce dose, or discontinue as necessary. 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 or moderate 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, nausea, thrombocytopenia, rash, vomiting, abdominal pain, anemia, pyrexia, abnormal LFTs, fatigue, cough, headache, edema; cardiac failure, left ventricular dysfunction, fluid retention, hepatic or renal toxicity.
Generic Drug Availability:
Tabs 100mg—120; 400mg, 500mg—30