nilotinib at a glance
Medicine class
BCR-ABL tyrosine kinase inhibitor
Main use
Philadelphia chromosome-positive CML in adults and eligible children
Food
Take on an empty stomach; food substantially increases absorption
Monitoring
Requires blood tests, heart-rhythm assessment and metabolic monitoring
What is nilotinib used for?
UK-licensed uses represented by the selected product are:
Newly diagnosed Philadelphia chromosome-positive CML in chronic phase in adults and eligible children.
Philadelphia chromosome-positive CML in chronic phase that is resistant to, or not tolerated with, previous treatment including imatinib, in adults and eligible children.
Philadelphia chromosome-positive CML in accelerated phase that is resistant to, or not tolerated with, previous treatment including imatinib, in adults. Evidence in blast crisis is unavailable.
How does nilotinib work?
In Philadelphia chromosome-positive CML, the abnormal BCR-ABL enzyme continually signals blood-forming cells to grow. Nilotinib binds to its ATP-binding site, reducing these growth signals and promoting the death of affected leukaemia cells.
nilotinib preparations and strengths
Capsule
Route: Oral
Strengths: 150 mg, 200 mg
How to take nilotinib
Follow the specialist’s prescription and treatment plan.
Swallow the capsules whole with water.
Do not eat for two hours before taking nilotinib or for at least one hour afterwards.
Avoid grapefruit juice and other grapefruit products.
If swallowing is difficult, the capsule contents may be mixed with one teaspoon of puréed apple and taken immediately. Do not use another food or a larger amount.
nilotinib side effects
Common or expected effects
- Rash, itching or hair loss
- Headache, tiredness or dizziness
- Nausea, vomiting, constipation, diarrhoea or abdominal discomfort
- Muscle, joint, back or limb pain
- Cough or upper respiratory infection
- Changes in blood counts, bilirubin, liver tests, glucose, cholesterol or electrolytes
Get urgent medical advice
- Fever or infection associated with reduced white blood cells
- Unusual bleeding or bruising associated with reduced platelets
- Palpitations, fainting or other symptoms of abnormal heart rhythm
- Chest pain, stroke symptoms or reduced circulation in a limb
- Severe breathlessness, swelling or rapid unexplained weight gain
- Severe abdominal pain suggesting pancreatitis
- Jaundice or other signs of liver injury
- Severe allergic reaction
nilotinib in pregnancy
Pregnancy data are limited, and animal studies indicate potential fetal harm. Nilotinib should generally be avoided in pregnancy unless specialist assessment finds treatment necessary. People who could become pregnant should use highly effective contraception during treatment and for two weeks afterwards, and discuss pregnancy plans promptly with their haematology team.
nilotinib while breastfeeding
It is unknown whether nilotinib enters human milk, and harm to a breastfed child cannot be excluded. Breastfeeding is not recommended during treatment or for two weeks after the last dose.
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.
Common questions about nilotinib
Answers are fully visible for fast scanning and source review.
Why must nilotinib be taken without food?
Food increases nilotinib absorption, which can raise blood concentrations and the risk of adverse effects, including abnormal heart rhythms.
Can I open nilotinib capsules if I cannot swallow them?
The selected capsule may be opened and its contents mixed with one teaspoon of puréed apple, then 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.