% and less than 10% - pericardial effusion; 0.1% and less than 1% - pericarditis
Ear and Labyrinth Disorders: 1% and less than 10% - tinnitus
Gastrointestinal Disorders: 1% and less than 10% - gastritis; 0.1% and less than 1% - acute pancreatitis, gastrointestinal hemorrhage1
General Disorders and Administrative Site Conditions: 1% and less than 10% - chest pain2, pain
Hepatobiliary Disorders: 1% and less than 10% - hepatotoxicity3, abnormal hepatic function4; 0.1% and less than 1% - liver injury
Immune System Disorders: 1% and less than 10% - drug hypersensitivity; 0.1% and less than 1% - anaphylactic shock
Infections and Infestations: 1% and less than 10% - pneumonia5, influenza, bronchitis
Investigations: 1% and less than 10% - electrocardiogram QT prolonged, increased blood creatine phosphokinase, increased blood creatinine
Metabolism and Nutrition Disorder: 1% and less than 10% - hyperkalemia, dehydration
Musculoskeletal and Connective Tissue Disorder: 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 renal failure, renal failure
Respiratory, Thoracic and Mediastinal Disorders: 1% and less than 10% - pleural effusion; 0.1% and less than 1% - acute pulmonary edema, respiratory failure, pulmonary hypertension
Skin and Subcutaneous Disorders: 1% and less than 10% - urticaria, pruritus, acne; 0.1% and less than 1% - erythema multiforme, exfoliative rash, drug eruption
1
Gastrointestinal hemorrhage includes the following preferred terms: gastrointestinal hemorrhage, gastric hemorrhage, upper gastrointestinal hemorrhage
2
Chest pain includes the following preferred terms: chest pain, chest discomfort
3
Hepatotoxicity includes the following preferred terms: hepatoxicity, toxic hepatitis, cytolytic hepatitis
4
Abnormal hepatic function includes the following preferred terms: abnormal hepatic function, liver disorder
5
Pneumonia includes the following preferred terms: pneumonia, bronchopneumonia, lobar pneumonia, primary atypical pneumonia
Drug Interactions
Drugs That May Increase Bosutinib Plasma Concentrations
CYP3A or P-glycoprotein (P-gp) inhibitors: Avoid the concomitant use of strong or moderate CYP3A and/or P-gp inhibitors with Bosulif as an increase in bosutinib plasma concentration is expected [see Dosage and Administration (2.5)]. In a dedicated cross-over drug-interaction trial in healthy volunteers (N=24), concomitant ketoconazole (strong CYP3A inhibitor) increased bosutinib Cmax 5.2-fold and AUC 8.6-fold compared to Bosulif alone [see Clinical Pharmacology (12.3)].
Drugs That May Decrease Bosutinib Plasma Concentrations
CYP3A Inducers: Avoid the concomitant use of strong or moderate CYP3A inducers with Bosulif as a large reduction in exposure is expected [see Dosage and Administration (2.6)]. In a dedicated cross-over drug-interaction trial in healthy volunteers (N=24), concomitant rifampin (strong CYP3A inducer) decreased bosutinib Cmax by 86% and AUC by 94% compared to Bosulif alone [see Clinical Pharmacology (12.3)].
Proton Pump Inhibitors: In a dedicated cross-over drug-interaction trial in healthy volunteers (N=24), concomitant lansoprazole (PPI) decreased bosutinib Cmax by 46% and AUC by 26% compared to Bosulif alone [see Clinical Pharmacology (12.3)].
Consider using short-acting antacids or H2 blockers instead of PPIs to avoid a reduction in bosut |
