Slideshows Images Quizzes

Copyright © 2018 by RxList Inc. RxList does not provide medical advice, diagnosis or treatment. See additional information.

Bosulif

Last reviewed on RxList: 1/21/2021
Bosulif Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

What Is Bosulif?

Bosulif (bosutinib) is a kinase inhibitor used to treat adult patients with chronic accelerated or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy.

What Are Side Effects of Bosulif?

Common side effects of Bosulif include:

Dosage for Bosulif

The recommended dose and schedule of Bosulif is 500 mg orally once daily with food.

What Drugs, Substances, or Supplements Interact with Bosulif?

Bosulif may interact with ketoconazole, rifampin, proton pump inhibitors, St. John's wort, and digoxin. Tell your doctor all medications and supplements you use.

Bosulif During Pregnancy and Breastfeeding

Bosulif is not recommended for use during pregnancy. It may harm a fetus. Women should use contraception to prevent pregnancy during and for at least 30 days after completing treatment with Bosulif. Because of potential risk to a nursing infant, breastfeeding is not recommended; consult your doctor.

Additional Information

Our Bosulif (bosutinib) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

QUESTION

What is leukemia? See Answer
Bosulif Consumer Information

3 pharmacies near 20147 have coupons for Bosulif (Brand Names:Bosulif for 120 Tablets)

CVS Pharmacy
CVS Pharmacy
$17552.19

Est. Regular Price

$16927.51

with free coupon

View Coupon
Walgreens
Walgreens
$17552.19

Est. Regular Price

$17317.97

with free coupon

View Coupon
Harris Teeter Pharmacy
Harris Teeter Pharmacy
$17552.19

Est. Regular Price

$17515.45

with free coupon

View Coupon

Get emergency medical help if you have signs of an allergic reaction: hives, itching; dizziness; back pain, joint pain; difficult breathing; swelling of your face, lips, tongue, or throat.

Stop using bosutinib and call your doctor at once if you have:

  • severe or ongoing nausea, vomiting, stomach pain, or diarrhea;
  • blood in your stools;
  • urinating more or less than usual;
  • swelling in your hands or feet, rapid weight gain;
  • feeling light-headed or short of breath;
  • low blood cell counts--fever, chills, tiredness, flu-like symptoms, mouth sores, skin sores, easy bruising, unusual bleeding, pale skin, cold hands and feet;
  • liver problems--upper stomach pain, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or
  • swelling or fluid build-up in the lungs--anxiety, sweating, pain when you breathe, feeling short of breath while lying down, wheezing, gasping for breath, cough with foamy mucus, chest pain, fast or uneven heart rate.

Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.

Common side effects may include:

  • headache, feeling tired;
  • nausea, vomiting, diarrhea, stomach pain;
  • fever, cough;
  • swelling;
  • rash; or
  • pale skin, bruising or bleeding.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Bosulif (Bosutinib Tablets)

SLIDESHOW

Signs of Cancer in Men: Could it Be Cancer? See Slideshow
Bosulif Professional Information

SIDE EFFECTS

The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling:

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Serious adverse reactions reported include anaphylactic shock [see CONTRAINDICATIONS], myelosuppression, gastrointestinal toxicity (diarrhea), fluid retention, hepatotoxicity and rash.

Adverse Reactions In Patients With Newly-Diagnosed CP CML

The clinical trial randomized and treated 533 patients with newly-diagnosed CP CML to receive BOSULIF 400 mg daily or imatinib 400 mg daily as single agents (Newly-Diagnosed CP CML Study) [see Clinical Studies]. The safety population (received at least 1 dose of BOSULIF) included:

  • two hundred sixty-eight (268) patients with newly-diagnosed CP CML had a median duration of BOSULIF treatment of 14.1 months (range: 0.3 to 24.7 months) and a median dose intensity of 391.8 mg/day.

Adverse reactions reported for greater than or equal to 20% of bosutinib patients with newly-diagnosed CML (N=268) were diarrhea (70%), nausea (35%), thrombocytopenia (35%), rash (34%), increased ALT (31%), abdominal pain (25%), and increased AST (23%) [see Clinical Studies].

Table 4 identifies adverse reactions greater than or equal to 10% for All Grades and Grades 3 or 4 (3/4) for the Phase 3 CP CML safety population.

Table 4: Adverse Reactions (10% or Greater) in Patients With Newly-Diagnosed CML in Bosutinib 400 mg Study

Adverse Reaction Bosutinib 400 mg Chronic Phase
CML
N=268
Imatinib 400 mg Chronic Phase
CML
N=265
All Grades
(%)
Grade 3/4
(%)
All Grades
(%)
Grade 3/4
(%)
Diarrhea 70 8 34 <1
Nausea 35 0 38 0
Thrombocytopenia* 35 14 20 6
Rash 34 1 21 2
Alanine aminotransferase increased 31 19 6 2
Abdominal pain 25 2 15 <1
Aspartate aminotransferase increased 23 10 6 2
Anemia§ 19 3 19 5
Headache 19 1 13 1
Fatigue 19 <1 19 0
Vomiting 18 1 16 0
Lipase increased# 13 10 8 5
Pyrexia 13 <1 8 0
Respiratory tract infectionÞ 12 <1 12 <1
Neutropeniaß 11 7 21 12
Arthralgia 11 <1 13 0
Asthenia 11 0 6 0
Appetite decreased 10 <1 6 0
Abbreviation: CML=Chronic myelogenous leukemia, N=number of patients.
* Thrombocytopenia includes the following preferred terms: Platelet count decreased, Thrombocytopenia.
Rash includes the following preferred terms: Acne, Dermatitis, Dermatitis acneiform, Dermatitis allergic, Dermatitis exfoliative, Drug reaction with eosinophilia and systemic symptoms, Photosensitivity reaction, Rash, Rash erythematous, Rash generalised, Rash macular, Rash maculo-papular, Rash papular, Rash pruritic, Urticaria.
Abdominal pain includes the following preferred terms: Abdominal discomfort, Abdominal pain, Abdominal pain lower, Abdominal pain upper, Abdominal tenderness, Gastrointestinal pain.
§ Anemia includes the following preferred terms: Anemia, Hemoglobin decreased
Fatigue includes the following preferred terms: Fatigue, Malaise.
# Lipase increased includes the following preferred terms: Hyperlipasemia, Lipase increased.
Þ Respiratory tract infection includes the following preferred terms: Lower respiratory tract infection, Respiratory tract infection, Respiratory tract infection viral, Upper respiratory tract infection, Viral upper respiratory tract infection.
ß Neutropenia includes the following preferred terms: Neutropenia, Neutrophil count decreased.

In the randomized study in patients with newly-diagnosed CP CML, one patient in the group treated with BOSULIF experienced a Grade 3 QTc prolongation (>500 msec). Patients with uncontrolled or significant cardiovascular disease including QT interval prolongation were excluded by protocol.

Table 5 identifies the clinically relevant or severe Grade 3/4 laboratory test abnormalities for the Phase 3 newly-diagnosed CML safety population.

Table 5: Number (%) of Patients With Clinically Relevant or Grade 3/4 Laboratory Test Abnormalities in Patients With Newly-Diagnosed CML in Bosutinib 400 mg Study, Safety Population

  Bosutinib
Chronic Phase CML
N=268
n (%)
Imatinib
Chronic Phase CML
N=265
n (%)
Hematology Parameters  
  Platelet Count (Low) less than 50×109/L 38 (14.2) 17 (6.4)
  Absolute Neutrophil Count less than 1×109/L 24 (9.0) 49 (18.5)
  Hemoglobin (Low) less than 80 g/L 19 (7.1) 15 (5.7)
  White Blood Cell Count (Low) less than 2×109/L 15 (5.6) 20 (7.5)
Biochemistry Parameters  
  SGPT/ALT greater than 5.0×ULN 62 (23.1) 7 (2.6)
  SGOT/AST greater than 5.0×ULN 32 (11.9) 8 (3.0)
  Lipase greater than 2×ULN 35 (13.1) 16 (6.0)
  Phosphorus (Low) less than 0.6 mmol/L 12 (4.5) 45 (17.0)
  Total Bilirubin greater than 3.0×ULN 3 (1.1) 2 (0.8)
  Amylase greater than 2×ULN 6 (2.2) 4 (1.5)
  Creatinine greater than 3.0×baseline; greater than 3.0×ULN 0 2 (0.8)
Abbreviations: ALT=alanine aminotransferase; AST=aspartate aminotransferase; CML=chronic myelogenous leukemia; SGPT=serum glutamic-pyruvic transaminase; SGOT=serum glutamicoxaloacetic transaminase; N/n=number of patients; ULN=upper limit of normal.

Adverse Reactions In Patients With Imatinib-Resistant Or -Intolerant Ph+ CP, AP, And BP CML

The single-arm clinical trial enrolled patients with Ph+ CP, AP, or BP CML and with resistance or intolerance to prior therapy [see Clinical Studies]. The safety population (received at least 1 dose of BOSULIF) included 546 CML patients:

  • two hundred eighty-four (284) patients with CP CML previously treated with imatinib only who had a median duration of BOSULIF treatment of 26 months, and a median dose intensity of 442 mg/day.
  • one hundred nineteen (119) patients with CP CML previously treated with both imatinib and at least 1 additional tyrosine kinase inhibitor (TKI) who had a median duration of BOSULIF treatment of 9 months and a median dose intensity of 442 mg/day.
  • one hundred forty-three (143) patients with advanced phase CML including 79 patients with AP CML and 64 patients with BP CML. In the patients with AP CML and BP CML, the median duration of BOSULIF treatment was 10 months and 3 months, respectively. The median dose intensity was 425 mg/day, and 456 mg/day, in the AP CML and BP CML cohorts, respectively.

Adverse reactions of any toxicity grade reported for greater than or equal to 20% of patients in the safety population of the single-arm trial in patients with CP CML (N=546) who were resistant or intolerant to prior therapy were diarrhea (85%), nausea (47%), abdominal pain (42%), rash (42%), thrombocytopenia (40%), vomiting (37%), anemia (27%), fatigue (26%), pyrexia (23%), cough (22%), headache (21%), ALT (20%), and edema (20%) [see Clinical Studies].

Table 6 identifies adverse reactions greater than or equal to 10% for All Grades and Grades 3 or 4 for the Phase 1/2 CML safety population based on long-term follow-up.

Table 6: Adverse Reactions (10% or Greater) in Patients With CML Who Were Resistant or Intolerant to Prior Therapy in Single-Arm Trial*

  Chronic Phase CML
N=403
Advanced Phase CML
N=143
All Grades
(%)
Grade 3/4
(%)
All Grades
(%)
Grade 3/4
(%)
Diarrhea 85 9 76 4
Nausea 47 1 48 2
Abdominal Pain 42 2 31 6
Rash 42 9 38 5
Thrombocytopenia§ 40 26 45 39
Vomiting 37 3 43 3
Anemia 27 11 38 27
Fatigue# 26 2 21 5
Pyrexia 23 <1 37 2
Cough 22 0 22 0
Headache 21 <1 17 4
Alanine aminotransferase increased 20 8 10 5
NeutropeniaÞ 18 12 22 20
Arthralgia 17 <1 14 0
Aspartate aminotransferase increased 16 3 11 3
Edemaß 20 1 17 2
Respiratory tract infectionà 15 <1 10 0
Decreased appetite 14 <1 13 0
Back pain 13 <1 8 1
Nasopharyngitis 13 0 6 0
Asthenia 13 2 10 <1
Pleural effusion 12 4 9 4
Dyspnea 12 2 20 6
Pruritus 12 <1 7 0
Dizziness 11 0 13 <1
Leukopeniaè 10 4 15 12
Blood creatinine increased 10 <1 6 <1
Influenza 10 <1 3 0
Chest painð 7 1 12 1
Abbreviations: CML=chronic myelogenous leukemia; N=number of patients.
Advanced Phase CML includes patients with Accelerated Phase and Blast Phase CML.
* Based on a Minimum of 48 Months of Follow-up.
Abdominal pain includes the following preferred terms: Abdominal discomfort, Abdominal pain, Abdominal pain lower, Abdominal pain upper, Abdominal tenderness, Gastrointestinal pain
Rash includes the following preferred terms: Acne, Dermatitis, Dermatitis acneiform, Dermatitis allergic, Drug eruption, Exfoliative rash, Photosensitivity reaction, Rash, Rash erythematous, Rash generalised, Rash macular, Rash maculo-papular, Rash papular, Rash pruritic, Urticaria
§Thrombocytopenia includes the following preferred terms: Platelet count decreased, Thrombocytopenia
Anemia includes the following preferred terms: Anemia, Hemoglobin decreased.
#Fatigue includes the following preferred terms: Fatigue, Malaise.
ÞNeutropenia includes the following preferred terms: Neutropenia, Neutrophil count decreased
ßEdema includes the following preferred terms containing: Edema, Edema peripheral, Face edema, Localized edema.
àRespiratory tract infection includes the following preferred terms: Lower respiratory tract infection, Respiratory tract infection, Respiratory tract infection viral, Upper respiratory tract infection, Viral upper respiratory tract infection.
è Leukopenia includes the following preferred terms: Leukopenia, White blood cell count decreased.
ð Chest pain included the following preferred terms: Chest discomfort, Chest pain.

In the single-arm study in patients with CML who were resistant or intolerant to prior therapy, 1 patient (0.2%) experienced QTcF interval of greater than 500 milliseconds. Patients with uncontrolled or significant cardiovascular disease including QT interval prolongation were excluded by protocol.

Table 7 identifies the clinically relevant or severe Grade 3/4 laboratory test abnormalities for the safety population of the study in patients with CML who were resistant or intolerant to prior therapy based on long-term follow-up.

Table 7: Number (%) of Patients With Clinically Relevant or Grade 3/4 Laboratory Test Abnormalities in the Safety Population of the Study of Patients With CML Who Were Resistant or Intolerant to Prior Therapy*

  Chronic Phase
(CP) CML
N=403
n (%)
Advanced Phase
(AdvP) CML
N=143
n (%)
All CP and AdvP
CML
N=546
n (%)
Hematology Parameters
  Platelet Count (Low) less than 50×109/L 105 (26) 82 (57) 187 (34)
  Absolute Neutrophil Count less than 1×109/L 65 (16) 55 (39) 120 (22)
  Hemoglobin (Low) less than 80 g/L 51 (13) 54 (38) 105 (19)
Biochemistry Parameters
  SGPT/ALT greater than 5.0×ULN 43 (11) 8 (6) 51 (9)
  SGOT/AST greater than 5.0×ULN 19 (5) 5 (4) 24 (4)
  Lipase greater than 2×ULN 42 (10) 9 (6) 51 (9)
  Phosphorus (Low) less than 0.6 mmol/L 30 (7) 10 (7) 40 (7)
  Total Bilirubin greater than 3.0×ULN 3 (1) 4 (3) 7 (1)
Abbreviations: ALT=alanine aminotransferase; AST=aspartate aminotransferase; CML=chronic myelogenous leukemia; N/n=number of patients; SGPT=serum glutamate-pyruvate transaminase; SGOT=serum glutamate-oxaloacetate aminotransferase; ULN=upper limit of normal.
* Based on a Minimum of 48 Months of Follow-up.

Additional Adverse Reactions From Multiple Clinical Trials

The following adverse reactions were reported in patients in clinical trials with BOSULIF (less than 10% of BOSULIF-treated patients). They represent an evaluation of the adverse reaction data from all 1272 patients with leukemia who received at least 1 dose of single-agent BOSULIF. These adverse reactions are presented by system organ class and are ranked by frequency. These adverse reactions are included based on clinical relevance and ranked in order of decreasing seriousness within each category.

Blood and Lymphatic System Disorders: less than 0.01% - Febrile neutropenia, Granulocytopenia

Cardiac Disorders: 1% and less than 10% - Pericardial effusion; 0.1% and less than 1% - Pericarditis

Ear and Labyrinth Disorders: 1% and less than 10% - Tinnitus

Vascular Disorders: 1% and less than 10% - Hypertension

Gastrointestinal Disorders: 1% and less than 10% - Gastritis; 0.1% and less than 1% - Pancreatitis (includes Pancreatitis, Pancreatitis acute), Gastrointestinal hemorrhage (includes Anal hemorrhage, Gastric hemorrhage, Gastrointestinal hemorrhage, Intestinal hemorrhage, Lower gastrointestinal hemorrhage, Rectal hemorrhage)

General Disorders and Administrative Site Conditions: 1% and less than 10% - Pain

Hepatobiliary Disorders: 1% and less than 10% - Hepatotoxicity (includes Hepatotoxicity, Hepatitis, Hepatitis toxic, Liver disorder), Hepatic function abnormal (includes Hepatic function abnormal, Liver function test abnormal, Transaminases increased); 0.1% and less than 1% - Liver injury (includes Liver injury, Drug-induced liver injury)

Immune System Disorders: 0.1% and less than 1% - Anaphylactic shock, Drug hypersensitivity

Infections and Infestations: 1% and less than 10% - pneumonia (includes pneumonia, atypical pneumonia), influenza, bronchitis

Investigations: 1% and less than 10% - Electrocardiogram QT prolonged (includes Electrocardiogram QT prolonged, Long QT syndrome), Blood bilirubin increased (includes Blood bilirubin increased, Hyperbilirubinaemia), Blood creatine phosphokinase increased, Amylase increased, GGT increased

Metabolism and Nutrition Disorders: 1% and less than 10% - Hypophosphatemia (includes Hypophosphatemia, Blood phosphorus decreased), Hyperkalemia (includes Hyperkalemia, Blood potassium increased), Dehydration

Musculoskeletal and Connective Tissue Disorders: 1% and less than 10% - Myalgia

Nervous System Disorders: 1% and less than 10% - Dysgeusia

Renal and Urinary Disorders: 1% and less than 10% - Acute kidney injury, Renal impairment, Acute renal failure, Renal failure

Respiratory, Thoracic and Mediastinal Disorders: 0.1% and less than 1% - Acute pulmonary edema, Respiratory failure, Pulmonary hypertension

Skin and Subcutaneous Disorders: 0.1% and less than 1% - Erythema multiforme

Post-Marketing Experience

The following additional adverse reactions have been identified during post-approval use of BOSULIF. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Blood and Lymphatic System Disorders: Thrombotic microangiopathy

Skin and Subcutaneous Tissue Disorders: Stevens-Johnson syndrome

Read the entire FDA prescribing information for Bosulif (Bosutinib Tablets)

Related Resources for Bosulif

Related Health

© Bosulif Patient Information is supplied by Cerner Multum, Inc. and Bosulif Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

QUESTION

What is leukemia? See Answer

Health Solutions From Our Sponsors