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Kinase inhibitor

Bosutinib (brand name BOSULIF) is a kinase inhibitor used to treat certain types of chronic myeloid leukemia (CML). It works by blocking specific proteins that help cancer cells grow.

How it worksBosutinib is a type of medicine called a tyrosine kinase inhibitor. It blocks the BCR-ABL protein and other proteins (Src, Lyn, and Hck) that help leukemia cells grow and survive.

Brand names:BOSULIF

Used for
Chronic phase Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML) in adults and children (1 year and older), whether newly diagnosed or resistant to other treatments.Accelerated phase or blast phase Ph+ CML in adults who have resistance or intolerance to other therapies.
Conditions
Chronic phase Philadelphia chromosome-positive chronic myelogenous leukemia (Ph+ CML)Accelerated phase Ph+ CMLBlast phase Ph+ CML
Class
Kinase InhibitorTyrosine-protein kinase inhibitorKinase inhibitorGastrointestinalHematologicHepaticCardiovascularRenal

How to take

FormsTablets (100 mg, 400 mg, 500 mg), Capsules (50 mg, 100 mg)
RoutesOral

Adults with newly diagnosed chronic phase CML usually take 400 mg once daily with food. Adults with resistant or intolerant chronic, accelerated, or blast phase CML usually take 500 mg once daily with food. Pediatric doses are based on body surface area.

Swallow tablets whole; do not cut, crush, break, or chew them. Capsules can be opened and mixed with applesauce or yogurt if they are difficult to swallow whole.

Key warnings

  • ·Monitor for liver toxicity by checking liver enzymes regularly.
  • ·Monitor blood counts for signs of myelosuppression.
  • ·Watch for signs of gastrointestinal issues like severe diarrhea or vomiting.
  • ·Be aware of potential heart-related side effects and fluid retention.
  • ·Monitor kidney function.
  • ·Bosutinib can cause harm to an unborn baby; use effective birth control during treatment.

Do not use if

  • ·People with a history of hypersensitivity to bosutinib (including anaphylaxis).

Side effects

Common

DiarrheaAbdominal painVomitingNauseaRashFatigueHeadacheDecreased appetiteConstipation

Serious

  • ·Liver problems (Hepatotoxicity)
  • ·Low blood counts (Myelosuppression)
  • ·Gastrointestinal issues
  • ·Heart-related issues (Cardiovascular toxicity)
  • ·Fluid retention
  • ·Kidney problems (Renal toxicity)

Seek help if

  • ·Severe diarrhea
  • ·Signs of liver problems (like yellowing skin)
  • ·Signs of fluid retention (like swelling)
  • ·Signs of heart issues
  • ·Signs of low blood counts (like fever or unusual bruising)

Interactions

  • ·Avoid using bosutinib with strong or moderate CYP3A inhibitors.
  • ·Avoid using bosutinib with strong CYP3A inducers.
  • ·Avoid proton pump inhibitors (PPIs); use short-acting antacids or H2 blockers instead, and take them at least 2 hours apart from bosutinib.
FoodTake bosutinib once daily with food.

Special populations

PregnancyBosutinib can cause fetal harm. It is recommended that women of reproductive age use effective contraception while taking this medicine.

PediatricBosutinib is approved for children 1 year of age and older with specific types of Ph+ CML.

GeriatricNo specific differences in safety or effectiveness were found in elderly patients, though older adults may be more sensitive to some side effects.

Talk to your doctor

Monitor

  • ·Liver enzymes
  • ·Blood counts
  • ·Renal function
  • ·Fluid retention
  • ·Gastrointestinal symptoms

Questions to ask

  • ·What are my target blood counts during treatment?
  • ·How often will my liver enzymes be checked?
  • ·What should I do if I experience severe diarrhea?
  • ·Which antacids are safe to take with my medication?

Pharmacokinetics

BioavailabilityBosutinib exhibits dose proportional increases in C max and AUC over the oral dose range of 200 to 800 mg.
MetabolismBosutinib is a CYP3A substrate.

Practical

OverdoseIf an overdose occurs, the patient should be monitored and given supportive treatment. No serious events were reported in clinical studies regarding overdose.

StorageStore at 20°C to 25°C (68°F to 77°F). Temporary excursions between 15°C and 30°F are allowed.

DisposalDispose of unused anticancer drugs according to local requirements. Avoid touching crushed or broken tablets.

Ingredients

Allergens

none

Inactive

croscarmellose sodiumiron oxide rediron oxide yellowmagnesium stearatemicrocrystalline cellulosepoloxamerpovidone K25polyvinyl alcoholtitanium dioxidepolyethylene glycol 3350talc

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-25.