Bosutinib at a glance
Medicine class
BCR-ABL tyrosine kinase inhibitor.
Main use
Philadelphia chromosome-positive chronic myeloid leukaemia.
Taking the tablets
Take with food and swallow whole with water.
Food to avoid
Avoid grapefruit and grapefruit juice because they can increase bosutinib exposure.
What is Bosutinib used for?
Bosutinib is licensed for adults with Ph+ CML.
Newly diagnosed chronic-phase Ph+ CML.
Chronic-, accelerated- or blast-phase Ph+ CML previously treated with one or more tyrosine kinase inhibitors, when imatinib, nilotinib and dasatinib are not considered appropriate.
How does Bosutinib work?
In Ph+ CML, the abnormal BCR-ABL protein sends continuous signals that drive production of leukaemia cells. Bosutinib blocks this tyrosine kinase and also inhibits several Src-family kinases, helping to limit abnormal-cell growth and survival.
Bosutinib preparations and strengths
Tablet
Route: Oral
Strengths: 100 mg, 400 mg, 500 mg
How to take Bosutinib
Follow the instructions supplied by the specialist cancer team.
Take the tablets with food.
Swallow film-coated tablets whole with water; do not cut, crush, break or chew them.
Avoid grapefruit and grapefruit juice.
Do not stop treatment without discussing it with the specialist team.
Bosutinib side effects
Common or expected effects
- Diarrhoea, nausea, vomiting or abdominal pain
- Tiredness, weakness, fever or headache
- Rash or itching
- Reduced appetite
- Swelling caused by fluid retention
- Cough, breathlessness or respiratory infection
- Reduced platelets, red blood cells or neutrophils
- Changes in liver, kidney or pancreatic blood tests
- Joint or back pain
Get urgent medical advice
- Fever or other evidence of infection, particularly with a low white-cell count
- Unusual bruising or bleeding
- Yellow skin or eyes, dark urine or right-sided upper abdominal pain
- Severe dehydration or persistent diarrhoea or vomiting
- New or worsening cough, painful breathing or breathlessness
- Chest pain, fainting, palpitations or an irregular heartbeat
- Painful spreading rash, blisters, peeling skin, or mouth or lip lesions
- Reduced urine, blood in the urine or flank pain
- Severe abdominal pain that may indicate pancreatitis
Bosutinib in pregnancy
Bosutinib is not recommended during pregnancy because human information is limited and animal studies indicate potential harm to the developing baby. Effective contraception is required during treatment and for at least one month afterwards; vomiting or diarrhoea may reduce absorption of oral contraceptives. Discuss pregnancy or plans to conceive promptly with the specialist team.
Bosutinib while breastfeeding
Breastfeeding should be stopped during bosutinib treatment because transfer into human milk is unknown and harm to the infant cannot be excluded. Discuss feeding options with the specialist team.
Bosutinib interactions
Ask the cancer team or pharmacist to check all prescription medicines, non-prescription products and herbal remedies. Important examples include:
Strong or moderate CYP3A inhibitors, including azole antifungals, clarithromycin, erythromycin, ritonavir, diltiazem and verapamil
May increase bosutinib exposure and adverse effects; concurrent use should generally be avoided or managed by the specialist.
CYP3A inducers, including rifampicin, carbamazepine, phenytoin, efavirenz, modafinil and St John's wort
May substantially reduce bosutinib exposure and effectiveness; concurrent use should generally be avoided.
Proton-pump inhibitors, such as omeprazole or lansoprazole
Can reduce bosutinib absorption; acid-suppression treatment should be reviewed by the specialist or pharmacist.
Common questions about Bosutinib
Answers are fully visible for fast scanning and source review.
Can bosutinib cause diarrhoea?
Yes. It can sometimes cause dehydration. Contact the cancer team if diarrhoea is severe, persistent, bloody or accompanied by reduced urine, dizziness or difficulty keeping fluids down.
Why are blood tests needed?
Bosutinib can reduce blood-cell counts and affect the liver, kidneys and pancreas. Blood tests help detect these effects and assess the CML response.
Can bosutinib reactivate hepatitis B?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.