bosutinib monohydrate at a glance
Medicine class
BCR-ABL tyrosine kinase inhibitor
Main role
Targeted treatment for Ph+ chronic myeloid leukaemia
Administration
Taken by mouth with food
Key practical point
Avoid grapefruit and grapefruit juice
What is bosutinib monohydrate used for?
Licensed uses represented by the selected products include:
Newly diagnosed chronic-phase Ph+ CML in adults and children aged 6 years and older.
Chronic-phase Ph+ CML in adults and children aged 6 years and older previously treated with at least one tyrosine kinase inhibitor, when imatinib, nilotinib and dasatinib are not considered appropriate.
Accelerated-phase or blast-phase Ph+ CML in adults previously treated with at least one tyrosine kinase inhibitor, when imatinib, nilotinib and dasatinib are not considered appropriate.
How does bosutinib monohydrate work?
Ph+ CML cells make an abnormal BCR-ABL enzyme that continuously signals them to grow. Bosutinib blocks this tyrosine kinase and also inhibits several Src-family kinases, reducing leukaemia-cell survival and multiplication.
bosutinib monohydrate preparations and strengths
Capsule
Route: Oral
Strengths: 50 mg, 100 mg
Tablet
Route: Oral
Strengths: 100 mg, 400 mg, 500 mg
How to take bosutinib monohydrate
Take bosutinib with food and follow the specialist team's instructions. Do not change or stop treatment without discussing it with them.
Swallow film-coated tablets whole with water; do not cut, crush, break or chew them.
Hard capsules may be swallowed whole.
If swallowing capsules is difficult, open them and mix the contents with applesauce or yoghurt. Consume the full mixture immediately without chewing and do not store it.
The soft-food mixture does not replace the required meal.
bosutinib monohydrate side effects
Common or expected effects
- Diarrhoea
- Nausea or vomiting
- Abdominal pain
- Rash
- Headache or dizziness
- Tiredness or fever
- Reduced appetite
- Cough or breathlessness
- Swelling caused by fluid retention
- Reduced red cells, white cells or platelets
- Raised liver or pancreatic enzymes
Get urgent medical advice
- Severe infection or fever associated with low white-cell counts
- Unexpected bleeding or extensive bruising
- Severe dehydration from diarrhoea or vomiting
- Liver injury, which may cause jaundice or dark urine
- Pancreatitis, suggested by severe persistent abdominal pain
- Fluid around the lungs or heart, pulmonary oedema or heart failure
- Heart ischaemia or an abnormal heart rhythm
- Severe allergic reaction
- Blistering or peeling skin reactions
- Acute kidney injury or worsening renal function
- Hepatitis B reactivation
bosutinib monohydrate in pregnancy
Bosutinib is not recommended during pregnancy because animal studies indicate reproductive toxicity and human data are limited. Effective contraception is advised during treatment and for at least 1 month after the last dose. Vomiting or diarrhoea may reduce absorption of oral contraceptives; seek prompt specialist advice if pregnancy occurs or is planned.
bosutinib monohydrate while breastfeeding
Breastfeeding should be stopped during bosutinib treatment because transfer into human milk is unknown and a risk to the infant cannot be excluded. Discuss feeding options with the specialist team.
bosutinib monohydrate interactions
A full medicines review is needed before treatment and whenever another medicine is started or stopped.
Strong or moderate CYP3A inhibitors, including clarithromycin, azole antifungals, ritonavir, verapamil and diltiazem
These can increase bosutinib exposure and adverse effects, so combined use should generally be avoided or managed by the specialist.
Strong or moderate CYP3A inducers, including rifampicin, carbamazepine, phenytoin and St John's wort
These can substantially reduce bosutinib exposure and may make treatment less effective, so combined use should generally be avoided.
Common questions about bosutinib monohydrate
Answers are fully visible for fast scanning and source review.
Is bosutinib monohydrate a type of chemotherapy?
It is a targeted anticancer treatment called a tyrosine kinase inhibitor, rather than traditional cytotoxic chemotherapy.
Can children take bosutinib monohydrate?
Selected formulations are licensed for chronic-phase Ph+ CML in children aged 6 years and older. Use is directed by a specialist paediatric haematology team.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.