[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/) › Nilotinib

# 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.

Updated Nov 1, 2026

## Quick facts

**Group**
[Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/)

**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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**BCR-ABL tyrosine kinase (ABL1 kinase domain)**Nilotinib

ⓘ The crystal shows nilotinib bound to the human ABL kinase domain in its inactive conformation.

**Target in 3D:** BCR-ABL tyrosine kinase (ABL1 kinase domain). PDB structure 3CS9 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/3CS9) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/chronic-myeloid-leukaemia/)

## Adverse effects

### Common

- Rash, itching
- Headache, fatigue
- Nausea, vomiting, diarrhoea, constipation
- Joint pain
- Raised bilirubin and lipase
- Night sweats

### Serious (rare, important)

- QT prolongation and sudden death (boxed warning)
- Myelosuppression
- Arterial occlusive events: heart attack, stroke, peripheral artery disease
- Pancreatitis
- Hepatotoxicity
- Electrolyte disturbances
- Bleeding and fluid retention

## 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.

## Memory aid

«NILotinib: NIL by mouth around the dose» (empty stomach), because food raises levels and the QT.

## 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.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/nilotinib/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**High alert**
An error with this medicine can cause serious harm: double checks and protocols are used.

## Connections

## Related drugs 2

- [Imatinib](https://durgical.com/en/pharmacology/imatinib/)
- [Dasatinib](https://durgical.com/en/pharmacology/dasatinib/)

## Related conditions 1

- [Chronic myeloid leukaemia](https://durgical.com/en/conditions/chronic-myeloid-leukaemia/)

[← Back to the class: Kinase inhibitors (targeted oncology)](https://durgical.com/en/pharmacology/classes/kinase-inhibitors/)

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](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e27c3e09-bc4f-4f01-be05-1c43ac72285d) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01EA03) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/) (World Health Organization, 2025).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/nilotinib/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/nilotinib/