Generic
Nilotinib
5 brands available in the market
At a glance
Nilotinib is a targeted cancer therapy used for Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML). It inhibits BCR-ABL tyrosine kinase to prevent cancer cell proliferation.
Description
Nilotinib is a potent inhibitor of BCR-ABL tyrosine kinase. It binds to and stabilises the inactive conformation of the kinase domain of Abl protein. It inhibits tyrosine kinase activity of the BCR-ABL oncogene which causes CML.
Indications
- Newly diagnosed Ph+ CML in chronic phase
- Imatinib-resistant or intolerant Ph+ CML (chronic phase and accelerated phase)
Therapeutic class
Targeted Cancer Therapy
Pharmacological class
BCR-ABL Tyrosine Kinase Inhibitor
Pharmacology
Nilotinib binds to the ATP-binding site of BCR-ABL tyrosine kinase with higher affinity than imatinib, overriding mutation-induced resistance. It stabilizes the inactive conformation of Abl protein's kinase domain to inhibit tyrosine kinase activity.
Mechanism of action
Prevents cancer cell proliferation by inhibiting BCR-ABL tyrosine kinase.
Dosage
Adult Dose (Oral):
- Newly diagnosed Ph+ CML-CP: 300 mg twice daily
- Resistant/intolerant Ph+ CML-CP & CML-AP: 400 mg twice daily
- Take on empty stomach (at least 2 hours before and 1 hour after food)
Administration
- Take on empty stomach (2 hours before and 1 hour after food)
- Swallow capsules whole with water
- Take approximately 12 hours apart
Missed dose
If you miss a dose, skip it and continue with normal schedule; do not double the dose.
Side effects
Common Side Effects:
- Rash, pruritus
- Headache, fever, fatigue
- Nausea, constipation, diarrhoea
- Alopecia, asthenia
- Muscle spasms, arthralgia, myalgia
- Insomnia, dizziness, vertigo
- Hepatotoxicity
- Myelosuppression (thrombocytopenia, neutropenia, anemia)
- QT prolongation
Precautions & warnings
- Risk of QT prolongation; correct electrolyte imbalances
- Correct hypokalaemia and hypomagnesaemia
- Monitor for hepatotoxicity
- Caution in history of pancreatitis
- Can cause fetal harm; use effective contraception
- Do not breastfeed
Contraindications
- Hypokalaemia, hypomagnesaemia or long QT syndrome
- Concurrent use with potent CYP3A4 inhibitors or antiarrhythmics
- Concurrent use with potent CYP3A4 inducers
- Pregnancy
Drug interactions
- Gastric acid secretion inhibitors (PPIs) may reduce solubility and bioavailability
- CYP3A4 inhibitors increase nilotinib serum levels
- CYP3A4 inducers decrease nilotinib serum levels
- QT prolonging drugs increase risk of QT prolongation
Food interactions
No harmful interaction with alcohol.
Use in pregnancy
Use in Pregnancy: Nilotinib is highly unsafe during pregnancy (Category D); definite evidence of severe fetal harm.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Nilotinib is unsafe during breastfeeding; may cause toxicity to the baby.
Pediatric use
Not recommended for children under 18 years.
Geriatric use
Elderly may require dose adjustment.
Renal / hepatic impairment
Renal Impairment: Safe in kidney disease; dose adjustment may not be needed.
Hepatic Impairment: Caution in liver disease; dose adjustment may be needed (lower starting dose based on hepatic impairment).
Overdose effects
Overdose: Neutropenia, vomiting and drowsiness; monitor and give supportive treatment.
Storage conditions
Store in a cool (not above 30°C) and dry place, away from light; keep out of reach of children.
Chemical structure
Nilotinib