BOSULIF

Bosutinib pharmacokinetics were assessed following oral dosing with food in adult patients with CML and were presented as geometric mean (CV%), unless otherwise specified. Bosutinib exhibits dose proportional increases in C max and AUC over the oral dose range of 200 to 800 mg (0.33 to 1.3 times the maximum approved recommended dosage of 600 mg). Bosutinib steady state C max was 127 ng/mL (31%), C trough was 68 ng/mL (39%) and AUC was 2370 ng

• h/mL (34%) following multiple oral doses of BOSULIF 4...

14.1 Adult Patients with Newly-Diagnosed CP Ph+ CML The efficacy of BOSULIF in patients with newly-diagnosed chronic phase Ph+ CML was evaluated in the B osutinib trial in F irst-line chr O nic myelogenous leukemia t RE atment (BFORE) Trial: "A Multicenter Phase 3, Open-Label Study of Bosutinib Versus Imatinib in Adult Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia" [NCT02130557]. The BFORE Trial is a 2-arm, open-label, randomized, multicenter trial conducted to investigate the efficacy and safety of BOSULIF 400 mg once daily alone compared with imatinib 400 mg once d...

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

• Gastrointestinal toxicity [see Warnings and Precautions (5.1) ] .
• Myelosuppression [see Warnings and Precautions (5.2) ] .
• Hepatic toxicity [see Warnings and Precautions (5.3) ] .
• Cardiovascular toxicity [see Warnings and Precautions (5.4) ] .
• Fluid retention [see Warnings and Precautions (5.5) ] .
• Renal toxicity [see Warnings and Precautions (5.6) ] .
• Most comm...

BOSULIF is contraindicated in patients with a history of hypersensitivity to BOSULIF. Reactions have included anaphylaxis [see Adverse Reactions (6.1) ] . Hypersensitivity to BOSULIF. ( 4 )

• 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 disco...

7 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 ) 7.1 Effect of Other Drugs on BOSULIF Strong or Moderate CYP3A Inhibitors Avoid the concomitant use of stron...