nilotinib hydrochloride monohydrate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
nilotinib hydrochloride monohydrate: clinical details
Prescribing considerations
- Initiation and ongoing management require a clinician experienced in CML.
- Review cardiovascular disease and risk factors, hepatic impairment, previous pancreatitis, gastrectomy, hepatitis B status and interacting medicines.
- Correct clinically important dehydration, hyperuricaemia, hypokalaemia and hypomagnesaemia before treatment.
- Reinforce fasting administration and grapefruit avoidance.
- Paediatric patients require growth monitoring and particular attention to hepatotoxicity.
Contraindications and cautions
- Hypersensitivity to nilotinib or any capsule excipient.
- Use particular caution with QT prolongation, significant cardiac disease, hepatic impairment or a history of pancreatitis.
- Capsules contain lactose and are unsuitable for specified rare hereditary disorders of galactose metabolism or absorption.
Monitoring
- Full blood count and molecular response using validated BCR-ABL testing.
- Baseline and clinically indicated ECG, with periodic potassium and magnesium assessment.
- Liver function, bilirubin and pancreatic enzymes.
- Blood glucose, lipid profile and cardiovascular status.
- Hepatitis B screening before treatment and monitoring of carriers.
- Growth and development in paediatric patients.
Clinical pharmacology
Nilotinib is an oral ATP-competitive inhibitor of BCR-ABL tyrosine kinase. It is primarily metabolised by CYP3A4, is a P-glycoprotein substrate, and can inhibit several metabolic enzymes including CYP3A4.
Formulation and product differences
- Selected products are hard gelatin capsules differing in size, colour and identifying imprint.
- All selected capsule strengths contain lactose monohydrate.
- For people unable to swallow capsules, contents may be dispersed only in apple sauce and taken immediately.
nilotinib hydrochloride monohydrate preparations and strengths
Capsule
Route: Oral
Strengths: 50 mg, 150 mg, 200 mg
nilotinib hydrochloride monohydrate interactions
The oncology or pharmacy team should check all prescribed, non-prescribed and herbal products. Important examples include:
Strong CYP3A4 inhibitors, including clarithromycin, azole antifungals and ritonavir
Can markedly increase nilotinib exposure and toxicity risk, including QT prolongation; combination should normally be avoided.
Strong CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John's wort
Can reduce nilotinib exposure and treatment effect; an alternative is generally needed.
Medicines that prolong the QT interval
Antiarrhythmics and medicines such as methadone, haloperidol or moxifloxacin can 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.