dasatinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
dasatinib: clinical details
Prescribing considerations
- Treatment should be initiated by a clinician experienced in diagnosing and treating leukaemia.
- Review the full medicines list for CYP3A4, gastric-acid suppression, QT-prolonging and bleeding interactions.
- Assess cardiopulmonary symptoms and risk factors before treatment; consider echocardiography where cardiac or pulmonary risk is present.
- Test for hepatitis B before treatment and obtain specialist input for positive serology.
- Use caution in hepatic impairment, significant cardiovascular disease, bleeding risk and patients predisposed to QT prolongation.
- Correct hypokalaemia or hypomagnesaemia before treatment.
Contraindications and cautions
- Hypersensitivity to dasatinib or any product excipient.
- The selected tablet contains lactose and should not be used in specified rare hereditary disorders of galactose handling.
Monitoring
- Full blood count, with intensity guided by disease phase, age and concurrent chemotherapy.
- Haematological, cytogenetic and molecular response as appropriate to the disease.
- New cough, dyspnoea, fatigue, oedema or chest symptoms; investigate for pleural effusion, pulmonary oedema, anaemia, cardiac dysfunction and pulmonary arterial hypertension.
- Bleeding, infection and thrombotic microangiopathy features.
- Cardiac function and ECG/electrolytes where clinically indicated by history, symptoms or interacting treatment.
- Patients with previous hepatitis B for reactivation during treatment and after its end.
- Bone growth and development in paediatric patients.
Clinical pharmacology
Dasatinib inhibits BCR-ABL in active and inactive conformations, SRC-family kinases and selected other oncogenic kinases. It is rapidly absorbed, highly protein-bound, metabolised mainly through CYP3A4 and eliminated predominantly in faeces as metabolites.
Formulation and product differences
- Film-coated tablets must be swallowed whole and must not be crushed, cut, chewed or dispersed.
- An oral-suspension formulation exists for selected patients unable to swallow tablets, but exposure differs and it is not directly interchangeable with tablets.
- The selected film-coated tablet contains lactose and is essentially sodium-free.
dasatinib preparations and strengths
Tablet
Route: Oral
Strengths: 20 mg, 50 mg, 80 mg, 100 mg, 140 mg
dasatinib interactions
Check all prescribed, non-prescribed and herbal products with the specialist pharmacist or prescriber. Important interactions include:
Strong CYP3A4 inhibitors, including clarithromycin, itraconazole, ketoconazole and ritonavir
These can increase dasatinib exposure and toxicity, so concurrent systemic use is generally avoided or requires specialist management.
CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John’s wort
These can substantially reduce dasatinib exposure and may make treatment less effective.
Proton-pump inhibitors and H2-receptor antagonists, including omeprazole and famotidine
Reduced stomach acidity can lower dasatinib absorption, so these medicines are not recommended with it.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.