Bosutinib
BOSULIF
What it isBCR-ABL and SRC tyrosine-kinase inhibitor; chronic myeloid leukemia.
Why this oneCompared with dasatinib or nilotinib, it has less pleural and arterial toxicity but much more early diarrhea.
What limits itDiarrhea can be dose-limiting; hepatotoxicity and CYP3A4 interactions require monitoring.
FDA-approved for
- chronic myeloid leukemia (2012)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Newly-diagnosed chronic phase Ph+ CML | Adults | 400 mg QD with food | 400 mg QD | 600 mg QD |
| CP/AP/BP Ph+ CML resistant or intolerant to prior therapy | Adults | 500 mg QD with food | 500 mg QD | 600 mg QD |
Titration Escalate by 100 mg increments if inadequate hematologic/cytogenetic/molecular response and no Grade ≥3 adverse reaction
Renal Reduced starting dose: CrCl 30–50 mL/min → 300 mg (newly-dx) / 400 mg (resistant) QD; CrCl <30 mL/min → 200 mg / 300 mg QD
Hepatic Reduce starting dose to 200 mg QD for any hepatic impairment (Child-Pugh A, B, or C)
Instructions
- Take once daily with food
- Swallow tablets whole; do not cut, crush, break, or chew
- If a dose is missed >12 h, skip it and take usual dose next day
- Continue until disease progression or intolerance
Cautions
- Gastrointestinal toxicity (diarrhea, nausea, vomiting, abdominal pain)
- Myelosuppression — monitor blood counts
- Hepatic toxicity — monitor liver enzymes monthly for first 3 months
- Cardiovascular toxicity
- Fluid retention
- Renal toxicity — monitor renal function
- Embryo-fetal toxicity
Adverse reactions
- Diarrhea, abdominal pain, vomiting, nausea
- Rash
- Fatigue
- Hepatic dysfunction
- Headache, pyrexia
- Respiratory tract infection
- Lab: ↑creatinine, ↓hemoglobin/platelets/ANC, ↑ALT/AST
Pregnancy Can cause fetal harm (animal data, mechanism); advise effective contraception; no human data
Lactation Advise women not to breastfeed
NO BOXED WARNINGS
Principal riskDiarrhea, dose-limiting early
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2025
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Bosutinib ballicule
