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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › BCR-ABL tyrosine kinase inhibitors
bosutinib
L01EA04
Forms & Strengths
- Oral tablets: 100 mg
- Oral tablets: 400 mg
- Oral tablets: 500 mg
Adult Dosing
- Newly diagnosed Philadelphia chromosome-positive (Ph+) CML: 400 mg orally once daily with food
- Chronic, accelerated, or blast phase Ph+ CML resistant or intolerant to prior therapy: 500 mg orally once daily with food
- Renal impairment adjustment (CrCl < 30 mL/min): Start at 300 mg daily for newly diagnosed, or 200 mg daily for resistant/intolerant CML
- Hepatic impairment adjustment: Start at 200 mg orally once daily
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of adult patients with newly diagnosed chronic phase Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML)
- Treatment of adult patients with chronic, accelerated, or blast phase Ph+ CML with resistance or intolerance to prior therapy
Mechanism of Action
- Dual SRC and ABL kinase inhibitor
- Inhibits the Bcr-Abl kinase, the abnormal protein produced by the Philadelphia chromosome in CML
- Inhibits multiple Src-family kinases including SRC, LCK, YES, and FYN
Contraindications
- Hypersensitivity to bosutinib or any of its excipients
- Baseline hepatic impairment (severe)
Adverse Reactions
- Diarrhea
- Nausea and vomiting
- Abdominal pain
- Rash
- Fatigue
- Thrombocytopenia and anemia
- Elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST)
- Edema
Drug Interactions
- Strong or moderate CYP3A inhibitors (e.g., ketoconazole, clarithromycin): Increase bosutinib exposure; avoid or reduce dose if co-administration is unavoidable
- Strong or moderate CYP3A inducers (e.g., rifampin, carbamazepine): Decrease bosutinib exposure; avoid co-administration
- Proton pump inhibitors (PPIs) and H2 blockers: May decrease bosutinib absorption; use short-acting antacids instead of PPIs
- Substrates of P-glycoprotein: Bosutinib may increase their plasma concentrations
Curated Content: Needs Vetting Before Put to Clinical Use