nilotinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
nilotinib: clinical details
Prescribing considerations
- Initiate under a clinician experienced in diagnosing and treating CML.
- Assess cardiac history, cardiovascular risk factors, concurrent medicines and adherence to fasting requirements.
- Test for hepatitis B before treatment; seek liver-disease expertise for positive serology and monitor carriers for reactivation.
- Use caution with hepatic impairment, previous pancreatitis, major cardiac disease, QT-risk factors or total gastrectomy.
- Correct clinically significant dehydration, hyperuricaemia, hypokalaemia and hypomagnesaemia before treatment.
- Monitor growth in paediatric patients.
Contraindications and cautions
- Hypersensitivity to nilotinib or any product excipient.
Monitoring
- Full blood count and differential.
- ECG and serum potassium and magnesium, particularly when QT risk is present.
- Liver function, bilirubin and serum lipase.
- Blood glucose and lipid profile.
- Cardiovascular status and modifiable vascular risk factors.
- Molecular response using validated BCR-ABL testing; stopping treatment requires specialist selection and intensive molecular monitoring.
Clinical pharmacology
Nilotinib is an oral BCR-ABL tyrosine kinase inhibitor. It is mainly metabolised through CYP3A4, is a P-glycoprotein substrate and can inhibit CYP3A4 and several other enzymes. Food increases its bioavailability, and QT prolongation is concentration-dependent.
Formulation and product differences
- The selected product is a hard gelatin capsule containing lactose.
- For swallowing difficulty, capsule contents may be dispersed only in a small amount of puréed apple and taken immediately.
nilotinib preparations and strengths
Capsule
Route: Oral
Strengths: 150 mg, 200 mg
nilotinib interactions
Check all prescribed, over-the-counter and herbal products with the cancer team or pharmacist.
Strong CYP3A4 inhibitors, including clarithromycin, itraconazole, voriconazole and ritonavir
Can substantially increase nilotinib exposure and the risk of toxicity, including QT prolongation; alternatives are generally preferred.
CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John’s wort
Can markedly reduce nilotinib exposure and potentially reduce treatment effectiveness.
QT-prolonging medicines, including amiodarone, sotalol, haloperidol, methadone and moxifloxacin
May add to the risk of a dangerous abnormal heart rhythm.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.