Bosutinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
Bosutinib: clinical details
Prescribing considerations
- Treatment should be initiated and supervised by a clinician experienced in CML.
- Review hepatic and renal function, cardiovascular and gastrointestinal history, concurrent medicines, hydration and tumour-lysis risk before treatment.
- Assess previous tyrosine kinase inhibitor response and intolerance against the licensed indication.
- Correct clinically significant dehydration, hyperuricaemia, hypokalaemia and hypomagnesaemia before treatment.
- Test for hepatitis B before treatment; obtain specialist hepatology advice for positive serology.
- Consider fertility counselling, including sperm conservation where appropriate.
Contraindications and cautions
- Hypersensitivity to bosutinib or a listed excipient.
- Hepatic impairment.
Monitoring
- Full blood count at baseline, frequently during early treatment and thereafter as clinically indicated.
- Liver function before treatment, monthly during the first three months and subsequently as indicated.
- Renal function at baseline and during treatment, particularly where renal impairment or risk factors are present.
- Assess diarrhoea, vomiting, hydration, infection, bleeding, fluid retention and pancreatic symptoms.
- Baseline ECG and subsequent QT assessment where clinically indicated; monitor potassium and magnesium.
- Monitor treatment response using appropriate haematological, cytogenetic and molecular assessments.
- Monitor hepatitis B carriers during treatment and for several months afterwards.
Clinical pharmacology
Bosutinib inhibits BCR-ABL and Src-family kinases. Absorption is increased by food and reduced when gastric pH rises. It is predominantly metabolised by CYP3A4 and mainly eliminated in faeces.
Formulation and product differences
- The selected product is a film-coated tablet containing bosutinib.
- Film-coated tablets should be swallowed whole and not cut, crushed, broken or chewed.
- Appearance, excipients, packaging and storage information may differ between manufacturers; verify the exact supplied pack.
Bosutinib preparations and strengths
Tablet
Route: Oral
Strengths: 100 mg, 400 mg, 500 mg
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.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.