Bosutinib

BOSULIF

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Pronunciation: boe-SYOO-ti-nib (BAH-su-lif)

Bosutinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Bosutinib ballicule

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.

Bosutinib molecular structure (skeletal formula) — Molecular structure: Bosutinib

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

Available strengths

cap 50, 100 mg
tab 100, 400, 500 mg

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

Cost

Bosutinib (BOSULIF)

Strength		#/mo	CostPlus
100 mg	tab	30 qd	not offered
400 mg	tab	30 qd	offered
500 mg	tab	30 qd	not offered
50 mg	cap	30 qd	not offered
100 mg	cap	30 qd	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Bosutinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2025

NO BOXED WARNINGS

Principal riskDiarrhea, dose-limiting early

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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