nilotinib hydrochloride monohydrate at a glance
Medicine class
BCR-ABL tyrosine kinase inhibitor
Main use
Philadelphia chromosome-positive chronic myeloid leukaemia in adults and eligible children
Food
Take on an empty stomach because food substantially increases absorption
Monitoring
Blood tests and checks of heart rhythm, electrolytes, liver, pancreas, glucose and lipids are needed
What is nilotinib hydrochloride monohydrate used for?
Licensed uses represented by the selected capsules include:
Newly diagnosed Philadelphia chromosome-positive CML in the chronic phase in adults and paediatric patients.
Chronic-phase or accelerated-phase Philadelphia chromosome-positive CML in adults when previous treatment, including imatinib, has not worked or was not tolerated.
Chronic-phase Philadelphia chromosome-positive CML in paediatric patients when previous treatment, including imatinib, has not worked or was not tolerated.
How does nilotinib hydrochloride monohydrate work?
In Philadelphia chromosome-positive CML, the abnormal BCR-ABL protein signals blood-forming cells to grow. Nilotinib blocks its tyrosine kinase activity, reducing survival and production of abnormal leukaemia cells.
nilotinib hydrochloride monohydrate preparations and strengths
Capsule
Route: Oral
Strengths: 50 mg, 150 mg, 200 mg
How to take nilotinib hydrochloride monohydrate
Follow the specialist team's prescription exactly. Food increases nilotinib exposure and can increase toxicity.
Swallow capsules whole with water.
Do not eat for at least two hours before taking it or for at least one hour afterwards.
Avoid grapefruit and grapefruit juice.
If swallowing is impossible, mix the contents of each capsule with one teaspoon of apple sauce and take immediately. Do not use another food or more apple sauce.
Do not stop treatment unless the specialist team advises this.
nilotinib hydrochloride monohydrate side effects
Common or expected effects
- Headache and fatigue
- Nausea, vomiting, diarrhoea, constipation or upper abdominal pain
- Rash, itching or hair loss
- Muscle, joint, back or limb pain
- Cough
- Reduced red cells or platelets
- Raised bilirubin, liver enzymes or pancreatic enzymes
Get urgent medical advice
- Abnormal heart rhythm or QT prolongation, with palpitations, dizziness or fainting
- Arterial blockage, heart attack or stroke symptoms
- Severe breathlessness, lung inflammation, or fluid around the lungs or heart
- Fever, severe infection, unusual bruising or bleeding caused by reduced blood cells
- Pancreatitis, suggested by severe upper abdominal pain
- Liver injury or hepatitis B reactivation
- Severe fluid retention with rapid weight gain or swelling
- Serious skin or allergic reactions
nilotinib hydrochloride monohydrate in pregnancy
Information in human pregnancy is limited, and animal studies found reproductive toxicity. Nilotinib should generally be avoided during pregnancy unless the woman's condition requires it. Anyone who is pregnant, could become pregnant or is planning pregnancy should speak to the specialist team promptly; highly effective contraception is advised during treatment and afterwards.
nilotinib hydrochloride monohydrate while breastfeeding
Breastfeeding is not recommended during treatment because a risk to the infant cannot be excluded. Published human experience is very limited, so feeding plans should be discussed with the oncology and maternity teams.
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.
Common questions about nilotinib hydrochloride monohydrate
Answers are fully visible for fast scanning and source review.
Why must nilotinib be taken without food?
Food substantially increases absorption and could raise blood concentrations to harmful levels.
Can nilotinib capsules be opened?
Only when swallowing is not possible. The contents may be mixed with one teaspoon of apple sauce and taken immediately; do not use another food.
Can I drink grapefruit juice while taking nilotinib?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.