Nilotinib
Kinase inhibitors (targeted oncology)
Kinase inhibitors (targeted oncology)High alert
An error with this medicine can cause serious harm: double checks and protocols are used.
A second-generation BCR-ABL inhibitor for CML. It prolongs the QT interval (boxed warning) and must be taken on an empty stomach.
Quick facts
- Group
- Kinase inhibitors (targeted oncology)
- Target
- BCR-ABL tyrosine kinase (ABL1 kinase domain)
- Key effects
- Rash · Headache · Nausea
- Monitor
- ECG at baseline · Potassium and magnesium · Lipase
- ATC
- L01EA03
No doses: the clinician sets them by the current guideline.
Mechanism of action
The crystal shows nilotinib bound to the human ABL kinase domain in its inactive conformation.
Nilotinib was designed from imatinib to fit the ABL kinase better: it binds and stabilises the inactive conformation of the ABL kinase domain and inhibits BCR-ABL more potently. It overcomes most imatinib-resistance mutations, but not T315I. It also inhibits PDGFR, KIT and DDR1.
- Fits the inactive ABL kinase pocket
- Stabilises the inactive conformation
- More potent BCR-ABL block than imatinib
- Covers most imatinib-resistance mutations (not T315I)
Indications
- Philadelphia-positive chronic myeloid leukaemia: newly diagnosed chronic phase, or chronic and accelerated phase after imatinib resistance or intolerance. Chronic myeloid leukaemia →
Adverse effects
Common
- Rash, itching
- Headache, fatigue
- Nausea, vomiting, diarrhoea, constipation
- Joint pain
- Raised bilirubin and lipase
- Night sweats
Contraindications
- Low potassium
- Low magnesium
- Long QT syndrome
Key interactions
- Other QT-prolonging drugs
- Avoided: additive QT prolongation.
- Strong CYP3A4 inhibitors
- Raise nilotinib levels and QT risk; avoided.
- Strong CYP3A4 inducers
- Lower its levels; avoided.
- Proton pump inhibitors
- Reduce absorption; short-acting antacids or H2 blockers are used instead, separated in time.
What is monitored
- ECG at baseline, a week after starting, periodically and after dose changes
- Potassium and magnesium, corrected before starting
- Blood counts
- Lipase, liver tests and bilirubin
- Cardiovascular risk factors
- BCR-ABL molecular response
Administration and safety
- Oral; swallowed whole at about the same time each day.
- Check the name carefully: kinase inhibitors with similar «-tinib» names are not interchangeable.
- Taken on an empty stomach: no food for two hours before and one hour after the dose.
Pregnancy and breastfeeding
Can harm the fetus; effective contraception is used and breastfeeding is not advised.
Nursing care
- Confirm the latest ECG and potassium and magnesium before refills.
- Ask about palpitations, fainting and chest or leg pain on walking.
- Ask about abdominal pain (pancreatitis).
- Teaching: strict fasting window around each dose, avoid grapefruit, report palpitations or fainting.
Pharmacokinetics
- Absorption
- Oral and incomplete; food markedly increases absorption (and QT risk), so food is avoided before and after each dose.
- Distribution
- Highly bound to plasma proteins.
- Metabolism
- Liver, mainly CYP3A4; it is a P-glycoprotein substrate and inhibitor.
- Half-life
- About 17 hours in patients.
Test yourself
Think of the answer, then tap the question to see it.
Why must nilotinib be taken on an empty stomach?
Food greatly increases its absorption, raising levels and the risk of QT prolongation.
Which three conditions contraindicate nilotinib?
Hypokalaemia, hypomagnesaemia and long QT syndrome.
Which BCR-ABL mutation does nilotinib not overcome?
T315I.
Connections
← Back to the class: Kinase inhibitors (targeted oncology)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - NILOTINIB capsule (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025).
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Representative model, for educational purposes only.