BOSULIF® Highlights

(bosutinib)

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use BOSULIF safely and effectively. See full prescribing information for BOSULIF.

BOSULIF (bosutinib) tablets, for oral use
BOSULIF (bosutinib) capsules, for oral use
Initial U.S. Approval: 2012

RECENT MAJOR CHANGES

Indications and Usage (1)

9/2023

Dosage and Administration, Recommended Dosing (2.1)

9/2023

Dosage and Administration, Dose Escalation (2.2)

9/2023

Dosage and Administration, Dosage Adjustments for Non-Hematologic Adverse Reactions (2.3)

9/2023

Dosage and Administration, Dosage Adjustments for Myelosuppression (2.4)

9/2023

Dosage and Administration, Dosage Adjustments for Renal Impairment or Hepatic Impairment (2.5)

9/2023

Warnings and Precautions, Gastrointestinal Toxicity (5.1)

9/2023

Warnings and Precautions, Hepatic Toxicity (5.3)

9/2023

Warnings and Precautions, Cardiovascular Toxicity (5.4)

9/2023

Warnings and Precautions, Fluid Retention (5.5)

9/2023

Warnings and Precautions, Renal Toxicity (5.6)

9/2023

INDICATIONS AND USAGE

BOSULIF is a kinase inhibitor indicated for the treatment of

•
adult and pediatric patients 1 year of age and older with chronic phase Ph+ chronic myelogenous leukemia (CML), newly-diagnosed or resistant or intolerant to prior therapy. (1)
•
adult patients with accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy. (1)

DOSAGE AND ADMINISTRATION

•
Adult patients with newly-diagnosed chronic phase Ph+ CML: 400 mg orally once daily with food. (2.1)
•
Adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy: 500 mg orally once daily with food. (2.1)
•
Pediatric patients with newly-diagnosed chronic phase Ph+ CML: 300 mg/m2 orally once daily with food. (2.1)
•
Pediatric patients with chronic phase Ph+ CML with resistance or intolerance to prior therapy: 400 mg/m2 orally once daily with food. (2.1)
•
Consider dose escalation by increments of 100 mg once daily to a maximum of 600 mg daily in adult patients who do not reach complete hematologic, cytogenetic, or molecular response and do not have Grade 3 or greater adverse reactions. (2.2)
•
Consider dose escalation by increments of 50 mg for those with a BSA <1.1 m2 and 100 mg for those with a BSA ≥1.1 m2 to a maximum of 600 mg daily in pediatric patients who do not reach sufficient response after 3 months. (2.2)
•
Adjust dosage for toxicity and organ impairment (2)

DOSAGE FORMS AND STRENGTHS

•
Tablets: 100 mg, 400 mg, and 500 mg. (3)
•
Capsules 50 mg, 100 mg. (3)

CONTRAINDICATIONS

Hypersensitivity to BOSULIF. (4)

WARNINGS AND PRECAUTIONS

•
Gastrointestinal Toxicity: Monitor and manage as necessary. Withhold, dose reduce, or discontinue BOSULIF. (2.3, 5.1)
•
Myelosuppression: Monitor blood counts and manage as necessary. Withhold, dose reduce, or discontinue BOSULIF. (2.4, 5.2)
•
Hepatic Toxicity: Monitor liver enzymes at least monthly for the first 3 months and as needed. Withhold, dose reduce, or discontinue BOSULIF. (2.3, 5.3)
•
Cardiovascular Toxicity: Monitor and manage as necessary. Interrupt, dose reduce, or discontinue BOSULIF. (5.4)
•
Fluid Retention: Monitor patients and manage using standard of care treatment. Interrupt, dose reduce, or discontinue BOSULIF. (2.3, 5.5)
•
Renal Toxicity: Monitor patients for renal function at baseline and during therapy with BOSULIF. (5.6)
•
Embryo-Fetal Toxicity: BOSULIF can cause fetal harm. Advise female patients of reproductive potential of potential risk to a fetus and to use effective contraception. (5.7)

ADVERSE REACTIONS

•
Most common adverse reactions (≥20%), in adult and pediatric patients with CML are diarrhea, abdominal pain, vomiting, nausea, rash, fatigue, hepatic dysfunction, headache, pyrexia, decreased appetite respiratory tract infection, and constipation. The most common laboratory abnormalities (≥20%) in adult and pediatric patients are creatinine increased, hemoglobin decreased, lymphocyte count decreased, platelets decreased, ALT increased, calcium decreased, white blood cell count decreased, AST increased, absolute neutrophil count decreased, glucose increased, phosphorus decreased, urate increased, alkaline phosphatase increased, lipase increased, creatine kinase increased, and amylase increased. (6.1)

To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

•
Strong and Moderate CYP3A Inhibitors: Avoid concomitant use with BOSULIF. (7.1)
•
Strong CYP3A Inducers: Avoid concomitant use with BOSULIF. (7.1)
•
Proton Pump Inhibitors: Use short-acting antacids or H2 blockers as an alternative to proton pump inhibitors. (7.1)

USE IN SPECIFIC POPULATIONS

Lactation: Advise women not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.

Revised: 9/2023

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Highlights

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use BOSULIF safely and effectively. See full prescribing information for BOSULIF.

BOSULIF (bosutinib) tablets, for oral use
BOSULIF (bosutinib) capsules, for oral use
Initial U.S. Approval: 2012

RECENT MAJOR CHANGES

Indications and Usage (1)

9/2023

Dosage and Administration, Recommended Dosing (2.1)

9/2023

Dosage and Administration, Dose Escalation (2.2)

9/2023

Dosage and Administration, Dosage Adjustments for Non-Hematologic Adverse Reactions (2.3)

9/2023

Dosage and Administration, Dosage Adjustments for Myelosuppression (2.4)

9/2023

Dosage and Administration, Dosage Adjustments for Renal Impairment or Hepatic Impairment (2.5)

9/2023

Warnings and Precautions, Gastrointestinal Toxicity (5.1)

9/2023

Warnings and Precautions, Hepatic Toxicity (5.3)

9/2023

Warnings and Precautions, Cardiovascular Toxicity (5.4)

9/2023

Warnings and Precautions, Fluid Retention (5.5)

9/2023

Warnings and Precautions, Renal Toxicity (5.6)

9/2023

INDICATIONS AND USAGE

BOSULIF is a kinase inhibitor indicated for the treatment of

•
adult and pediatric patients 1 year of age and older with chronic phase Ph+ chronic myelogenous leukemia (CML), newly-diagnosed or resistant or intolerant to prior therapy. (1)
•
adult patients with accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy. (1)

DOSAGE AND ADMINISTRATION

•
Adult patients with newly-diagnosed chronic phase Ph+ CML: 400 mg orally once daily with food. (2.1)
•
Adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy: 500 mg orally once daily with food. (2.1)
•
Pediatric patients with newly-diagnosed chronic phase Ph+ CML: 300 mg/m2 orally once daily with food. (2.1)
•
Pediatric patients with chronic phase Ph+ CML with resistance or intolerance to prior therapy: 400 mg/m2 orally once daily with food. (2.1)
•
Consider dose escalation by increments of 100 mg once daily to a maximum of 600 mg daily in adult patients who do not reach complete hematologic, cytogenetic, or molecular response and do not have Grade 3 or greater adverse reactions. (2.2)
•
Consider dose escalation by increments of 50 mg for those with a BSA <1.1 m2 and 100 mg for those with a BSA ≥1.1 m2 to a maximum of 600 mg daily in pediatric patients who do not reach sufficient response after 3 months. (2.2)
•
Adjust dosage for toxicity and organ impairment (2)

DOSAGE FORMS AND STRENGTHS

•
Tablets: 100 mg, 400 mg, and 500 mg. (3)
•
Capsules 50 mg, 100 mg. (3)

CONTRAINDICATIONS

Hypersensitivity to BOSULIF. (4)

WARNINGS AND PRECAUTIONS

•
Gastrointestinal Toxicity: Monitor and manage as necessary. Withhold, dose reduce, or discontinue BOSULIF. (2.3, 5.1)
•
Myelosuppression: Monitor blood counts and manage as necessary. Withhold, dose reduce, or discontinue BOSULIF. (2.4, 5.2)
•
Hepatic Toxicity: Monitor liver enzymes at least monthly for the first 3 months and as needed. Withhold, dose reduce, or discontinue BOSULIF. (2.3, 5.3)
•
Cardiovascular Toxicity: Monitor and manage as necessary. Interrupt, dose reduce, or discontinue BOSULIF. (5.4)
•
Fluid Retention: Monitor patients and manage using standard of care treatment. Interrupt, dose reduce, or discontinue BOSULIF. (2.3, 5.5)
•
Renal Toxicity: Monitor patients for renal function at baseline and during therapy with BOSULIF. (5.6)
•
Embryo-Fetal Toxicity: BOSULIF can cause fetal harm. Advise female patients of reproductive potential of potential risk to a fetus and to use effective contraception. (5.7)

ADVERSE REACTIONS

•
Most common adverse reactions (≥20%), in adult and pediatric patients with CML are diarrhea, abdominal pain, vomiting, nausea, rash, fatigue, hepatic dysfunction, headache, pyrexia, decreased appetite respiratory tract infection, and constipation. The most common laboratory abnormalities (≥20%) in adult and pediatric patients are creatinine increased, hemoglobin decreased, lymphocyte count decreased, platelets decreased, ALT increased, calcium decreased, white blood cell count decreased, AST increased, absolute neutrophil count decreased, glucose increased, phosphorus decreased, urate increased, alkaline phosphatase increased, lipase increased, creatine kinase increased, and amylase increased. (6.1)

To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

•
Strong and Moderate CYP3A Inhibitors: Avoid concomitant use with BOSULIF. (7.1)
•
Strong CYP3A Inducers: Avoid concomitant use with BOSULIF. (7.1)
•
Proton Pump Inhibitors: Use short-acting antacids or H2 blockers as an alternative to proton pump inhibitors. (7.1)

USE IN SPECIFIC POPULATIONS

Lactation: Advise women not to breastfeed. (8.2)

See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.

Revised: 9/2023
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