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Bosulif

bosutinib
BCR-ABL/SRC Kinase Inhibitor Pfizer FDA Approved 2012
Indications Dosing Forms Contraindications Warnings Adverse Reactions Pharmacology Clinical Studies Tumor Types
1. Indications and Usage

Newly diagnosed chronic phase Ph+ CML in adults; Chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy in adults and pediatric patients ≥1 year.

2. Dosage and Administration

Newly diagnosed CML-CP: 400 mg orally once daily with food
Resistant/intolerant CML: 500 mg orally once daily with food
Dose escalation (CML-CP): May increase to 600 mg daily if inadequate response by Week 8
Hepatic impairment (Child-Pugh A): 200 mg; (Child-Pugh B/C): 100 mg

3. Dosage Forms and Strengths

Tablets: 100 mg, 200 mg, 400 mg, 500 mg

4. Contraindications

Hypersensitivity to bosutinib.

5. Warnings and Precautions
  • GI Toxicity: Diarrhea in 82% (Grade 3-4: 9%). Nausea 46%, vomiting 37%, abdominal pain 35%. Most within first month. Manage with antiemetics and antidiarrheals.
  • Myelosuppression: Grade 3-4 thrombocytopenia (25%), neutropenia (16%), anemia (8%). Monitor CBC weekly × 1 month, then monthly.
  • Hepatotoxicity: ALT/AST elevation in 22% (Grade 3-4: 9%). Monitor LFTs monthly × 3 months, then as needed.
  • Fluid Retention: Pleural effusion (8%), pericardial effusion (1%), peripheral edema (4%).
  • Renal Toxicity: Decline in eGFR in majority of patients. Monitor kidney function.
6. Adverse Reactions
Most Common Adverse Reactions

Diarrhea (82%), nausea (46%), vomiting (37%), abdominal pain (35%), thrombocytopenia (35%), rash (34%), fatigue (26%), pyrexia (22%), ALT elevation (22%), headache (19%), cough (15%), anemia (19%)

Diarrhea
82%
Nausea
46%
Vomiting
37%
Abdominal Pain
35%
Thrombocytopenia
35%
Rash
34%
Fatigue
26%
Pyrexia
22%
ALT elevation
22%
Headache
19%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

12. Clinical Pharmacology
Mechanism of Action

Bosutinib is a kinase inhibitor of BCR-ABL and SRC family kinases. It binds to and inhibits the kinase activity of BCR-ABL, including multiple imatinib-resistant mutant forms (but not T315I). Unlike imatinib and dasatinib, bosutinib has minimal activity against c-KIT and PDGFR, which may contribute to its distinct safety profile (less fluid retention, less myelosuppression).

Pharmacokinetics

Tmax: 4-6 hours. Half-life: approximately 22.5 hours. Protein binding: 94%. Metabolized by CYP3A4. Food increases AUC by 70% (take with food). Excreted primarily in feces (91%). Steady-state by Day 7.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
📋 All Bosutinib Trials on ClinicalTrials.gov ↗ 📚 PubMed: Bosutinib Clinical Trials ↗
Approved Tumor Types
Chronic Myeloid Leukemia