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Bosulif

Last reviewed on RxList: 4/27/2017
Bosulif Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

Last reviewed on RxList 05/2/2017

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. Common side effects of Bosulif include:

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

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.

Bosulif Consumer Information

Get emergency medical help if you have any of these signs of an allergic reaction: hives; 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;
  • black, bloody, or tarry stools, coughing up blood or vomit that looks like coffee grounds;
  • fever, chills, body aches, flu symptoms, sores in your mouth and throat;
  • pale skin, easy bruising, unusual bleeding (nose, mouth, vagina, or rectum), purple or red pinpoint spots under your skin;
  • upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • swelling in your hands or feet, rapid weight gain;
  • pain in your chest, on your left side, or behind your breastbone;
  • pain when you breathe, fast or uneven heart rate, feeling short of breath (especially when lying down);
  • anxiety, sweating, wheezing, gasping for breath, cough with foamy mucus; or
  • feeling weak, tired, dizzy, or light-headed.

Common side effects may include:

  • headache, dizziness, tired feeling;
  • mild stomach discomfort;
  • joint pain, back pain;
  • mild itching or rash; or
  • cold symptoms such as stuffy nose, sneezing, sore throat.

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)

Bosulif Professional Information

SIDE EFFECTS

The following 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 of any toxicity grade reported for greater than 20% of patients in Phase 1/2 trial (n=546) were diarrhea (82%), nausea (47%), thrombocytopenia (42%), rash (41%), vomiting (39%), abdominal pain (39%), respiratory tract infection (39%), anemia (30%), pyrexia (27%), liver test abnormalities (24%), fatigue (25%), cough (22%), and headache (20%) [see Clinical Studies].

Adverse Reactions In Patients With Imatinib-Resistant Or -Intolerant Ph+ Chronic Phase (CP), Accelerated Phase (AP),And Blast Phase (BP) CML

The single-arm Phase 1/2 clinical trial (Study 1) enrolled patients with Ph+ chronic, accelerated, or blast phase chronic myelogenous leukemia (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:

  • 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.
  • 119 patients with CP CML previously treated with both imatinib and at least 1 additional TKI who had a median duration of BOSULIF treatment of 9 months and a median dose intensity of 442 mg/day.
  • 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.

Table 3 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 3:Adverse Reactions (10% or Greater) in Patients with CML in Study 1*

  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 Paina 42 2 31 6
Thrombocytopeniab 40 26 45 39
Respiratory tract
infectionc
39 5 38 12
Vomiting 37 3 43 3
Rashd 42 8 38 4
Liver test abnormalitiese 26 9 20 10
Fatiguef 26 2 21 5
Anemiag 27 11 38 27
Pyrexia 23 <1 37 2
Headache 21 <1 17 4
Cough 22 0 22 0
Neutropeniah 18 12 22 20
Edemai 20 1 17 2
Arthralgia 17 <1 14 0
Decreased appetite 14 <1 13 0
Renal impairmentj 13 2 13 5
Back pain 13 <1 8 1
Asthenia 13 2 10 <1
Pruritus 12 <1 7 0
Dizziness 11 0 13 <1
Dyspnea 12 2 20 6
Pleural effusion 12 4 9 4
Leukopeniak 10 4 15 12
Chest painl 7 1 12 1
*Based on a Minimum of 48 Months of Follow-up
Advanced Phase CML includes patients with Accelerated Phase and Blast Phase CML
a Abdominal pain includes the following preferred terms: Abdominal discomfort, Abdominal pain, Abdominal pain lower, Abdominal pain upper, Abdominal tenderness, Gastrointestinal pain
b Thrombocytopenia includes the following preferred terms: Platelet count decreased, Thrombocytopenia
c Respiratory tract infection includes the following preferred terms: Acute sinusitis, Acute tonsillitis, Atypical pneumonia, Bronchitis, Bronchitis bacterial, Bronchitis pneumococcal, Bronchopneumonia, Chronic tonsillitis, H1N1 influenza, Influenza, Laryngitis, Lobar pneumonia, Lower respiratory tract infection, Lung infection, Nasopharyngitis, Pertussis, Pharyngitis, Pharyngotonsillitis, Pneumonia, Pneumonia bacterial, Pneumonia fungal, Pneumonia necrotising, Pneumonia pneumococcal, Pneumonia streptococcal, Pulmonary mycosis, Respiratory tract infection, Respiratory tract infection viral, Rhinitis, Sinusitis, Tonsillitis, Tonsillitis bacterial, Tracheitis, Upper respiratory tract infection, Viral upper respiratory tract infection
d Rash includes the following preferred terms: Acne, Dermatitis, Dermatitis acneiform, Dermatitis allergic, Eczema, Eczema asteatotic, Erythema, Generalised erythema, Intertrigo, Palmar erythema, Prurigo, Rash, Rash erythematous, Rash generalised, Rash macular, Rash maculopapular, Skin irritation, Stasis dermatitis
e Liver Test Abnormalities includes the following preferred terms: Alanine aminotransferase increased, Aspartate aminotransferase increased, Bilirubin conjugated increased, Blood alkaline phosphatase increased, Blood bilirubin increased, Blood bilirubin unconjugated increased, Gamma-glutamyltransferase increased, Hepatic enzyme increased, Hepatic function abnormal, Hyperbilirubinaemia, Liver function test abnormal, Transaminases increased
f Fatigue includes the following preferred terms: Fatigue, Malaise
gAnaemia includes the following preferred terms: Anaemia, Haemoglobin decreased
hNeutropenia includes the following preferred terms: Neutropenia, Neutrophil count decreased
i Edema includes the following preferred terms containing: Acute pulmonary edema, Allergic edema, Angioedema, Bone marrow edema, Circumoral edema, Eyelid edema, Eye edema, Face edema, Gastrointestinal edema, Localised edema, Edema, Edema peripheral, Periorbital edema, Pharyngeal edema, Pulmonary edema, Scrotal edema, Testicular edema, Tongue edema, Weight increased
j Renal impairment includes the following preferred terms: Acute kidney injury, Acute prerenal failure, Anuria, Blood creatinine abnormal, Blood creatinine increased, Chronic kidney disease, Oliguria, Prerenal failure, Renal failure, Renal impairment
k Leukopenia includes the following preferred terms: Leukopenia, White blood cell count decreased
l Chest pain included the following preferred terms: Chest pain, chest discomfort.

In the single-arm Phase 1/2 clinical trial, one 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 4 identifies the clinically relevant or severe Grade 3/4 laboratory test abnormalities for the Phase 1/2 CML safety population based on long-term follow-up.

Table 4:Number (%) of Patients with Clinically Relevant or Severe Grade 3/4 Laboratory Test Abnormalities in Patients with CML in Study 1, Safety Population*

  Chronic Phase CML
N=403
n (%)
Advanced Phase 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)
*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 881 patients with Ph+ 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: 1% and less than 10% - febrile neutropenia; less than 1% - 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, gastrointestinal hemorrhage (Anal hemorrhage, Gastric hemorrhage, Gastrointestinal hemorrhage, Hematemesis, Hematochezia, Intestinal hemorrhage, Lower gastrointestinal hemorrhage, Melena, Rectal hemorrhage, Upper gastrointestinal hemorrhage); 0.1% and less than 1% - acute pancreatitis

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

Hepatobiliary Disorders: 1% and less than 10% - hepatotoxicity (includes Allergic hepatitis, Ascites, Cholestasis, Drug-induced liver injury, Hepatic steatosis, Hepatitis toxic, Hepatocellular injury, Hepatotoxicity, Liver disorder, Liver injury)

Immune System Disorders: 1% and less than 10% - drug hypersensitivity; 0.1% and less than 1% - anaphylactic shock

Investigations: 1% and less than 10% - electrocardiogram QT prolonged (includes Electrocardiogram QT prolonged, Long QT syndrome), blood creatine phosphokinase increased, amylase increased.

Metabolism and Nutrition Disorder: 1% and less than 10% - hyperkalemia, dehydration, hypophosphatemia

Musculoskeletal and Connective Tissue Disorder: 1% and less than 10% - myalgia

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

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

Skin and Subcutaneous Disorders: 1% and less than 10% - urticaria, pruritus; 0.1% and less than 1% - erythema multiforme, exfoliative rash, drug eruption

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.

Skin and Subcutaneous Tissue Disorders: Stevens-Johnson syndrome

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

Related Resources for Bosulif

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© 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.

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