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Bosulif Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Tabs 100mg—120; 400mg, 500mg—30; Caps 50mg—30; 100mg—150
Manufacturer
Generic Availability
Mechanism of Action
Bosulif Indications
Indications
In adults and pediatric patients with chronic phase (CP) Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML), newly diagnosed or resistant or intolerant to prior therapy. In adults with accelerated phase (AP), or blast phase (BP) Ph+ CML with resistance or intolerance to prior therapy.
Bosulif Dosage and Administration
Adult
Take with food. Swallow tabs or caps whole. If unable to swallow caps whole, can open caps and mix contents with applesauce or yogurt. Continue until disease progression or patient intolerance. Newly-diagnosed CP Ph+ CML: 400mg once daily. Renal impairment (CrCl 30–50mL/min): initially 300mg daily; (CrCl <30mL/min): initially 200mg daily. CP, AP, or BP Ph+ CML 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.
Children
<18yrs (AP or BP Ph+ CML) or <1yr (CP Ph+ CML): not established. Take with food. Swallow tabs or caps whole. If unable to swallow caps whole, can open caps and mix contents with applesauce or yogurt. Continue until disease progression or patient intolerance. 1–17yrs: Newly diagnosed CP Ph+ CML: BSA (<0.55m2): 150mg once daily; (0.55–<0.75m2): 200mg once daily; (0.75–<0.9m2): 250mg once daily; (0.9–<1.1m2): 300mg once daily; (≥1.1m2): 400mg once daily. CP Ph+ CML resistant or intolerant to prior therapy: BSA (<0.55m2): 200mg once daily; (0.55–<0.63m2): 250mg once daily; (0.63–<0.75m2): 300mg once daily; (0.75–<0.9m2): 350mg once daily; (0.9–<1.1m2): 400mg once daily; (≥1.1m2): 500mg once daily. Renal/hepatic impairment, dose escalation or dose adjustments for toxicity: see full labeling.
Administration
Nursing Considerations
Take with food. If dose is missed beyond 12hrs, skip dose and take the usual dose on the following day. Contraceptive measures to prevent pregnancy should be used during and for at least 2 weeks after completing treatment.
Bosulif Contraindications
Not Applicable
Bosulif Boxed Warnings
Not Applicable
Bosulif Warnings/Precautions
Warnings/Precautions
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 CBCs 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).
Bosulif Pharmacokinetics
Absorption
Following administration of a single oral dose of Bosulif 500 mg with food in patients with CML, the median (minimum, maximum) time-to-peak concentration (tmax) was 6.0 (6.0, 6.0) hours. The absolute bioavailability was 34% in healthy subjects.
Effect of Food:
- When given with a high fat meal in healthy subjects, oral bosutinib Cmax increased 1.8-fold and AUC increased 1.7-fold. The high-fat meal (800–1000 total calories) consisted of approximately 150 protein calories, 250 carbohydrate calories, and 500–600 fat calories.
Distribution
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Mean volume of distribution (SD): 2441 (796) L in healthy subjects; 6080 (1230) L in patients with CML.
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Protein binding is 94% in vitro and 96% ex vivo.
Elimination
Fecal (91.3%), renal (3.3%). Mean half-life (SD): 22.5 (1.7) hours. Mean clearance (SD): 189 (48) L/h.
Bosulif Interactions
Interactions
Bosulif Adverse Reactions
Adverse Reactions
Diarrhea, rash, nausea, abdominal pain, vomiting, fatigue, hepatic dysfunction, respiratory tract infection, pyrexia, headache, decreased appetite, constipation, lab abnormalities; myelosuppression, pneumonia, pleural effusion, coronary artery disease, gastroenteritis.
Bosulif Clinical Trials
See Literature
Bosulif Note
Not Applicable
Bosulif Patient Counseling
See Literature
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