Treatment of newly diagnosed adult patients with Philadelphia chromosome–positive chronic myeloid leukemia (Ph+ CML) in the chronic phase. Long-term outcome data are still being evaluated.
It is also indicated for chronic phase (CP) and accelerated phase (AP) Ph+ CML in adult patients who are resistant to or intolerant of prior therapy including imatinib. However, clinical benefit such as improvement in disease-related symptoms or overall survival has not been fully established.
Chronic myelogenous leukemia (CML) is caused by the BCR-ABL oncogene. Nilotinib inhibits the tyrosine kinase activity of the BCR-ABL protein. It binds to the ATP-binding site of BCR-ABL with higher affinity than imatinib, thereby overcoming resistance caused by mutations. Nilotinib (AMN107) also inhibits TEL-platelet-derived growth factor receptor-beta (TEL-PDGFRβ), associated with chronic myelomonocytic leukemia, and FIP1-like-1-PDGFRα, associated with hypereosinophilic syndrome, suggesting potential use in certain myeloproliferative disorders. It also inhibits the c-KIT receptor kinase, including the D816V-mutated KIT variant, at clinically achievable concentrations, supporting its potential role in mastocytosis and gastrointestinal stromal tumors.
Recommended Dose: Newly diagnosed Ph+ CML-CP: 300 mg orally twice daily.
Resistant or intolerant Ph+ CML-CP and CML-AP: 400 mg orally twice daily.
Administer Nilotinib approximately 12 hours apart and must not take with food. Swallow the capsules whole with water. Do not consume food for at least 2 hours before the dose is taken and for at least one hour after. Dose adjustment may be required for hematologic and non-hematologic toxicities, and drug interactions. A lower starting dose is recommended in patients with hepatic impairment (at baseline).
Drugs that reduce gastric acid secretion (e.g. proton pump inhibitors) may decrease the solubility and bioavailability of Nilotinib.
Contraindicated in patients with hypokalaemia, hypomagnesaemia, or long QT syndrome. Concomitant use with potent CYP3A4 inhibitors, antiarrhythmic drugs, other QT-prolonging agents, and strong CYP3A4 inducers is not recommended.
May include rash, pruritus, hepatotoxicity, headache, fever, fatigue, gastrointestinal disturbances (nausea, constipation, diarrhea), alopecia, asthenia, muscle spasms, arthralgia, myalgia, musculoskeletal or chest pain, edema, folliculitis, papilloma, insomnia, dizziness, vertigo, anxiety, paresthesia, hyperhidrosis, dry skin, urticaria, acne, conjunctivitis, dry eye, flushing, dyspnea, cough, myelosuppression (thrombocytopenia, neutropenia, anemia), thrombotic events or hemorrhage, arrhythmias, heart failure, pericarditis, palpitations, hypertension, angina, myocardial infarction, elevated liver enzymes (AST/ALT), increased serum lipase, and electrolyte imbalance.
Pregnancy Category D. There is evidence of human fetal risk, but potential benefits may justify use in life-threatening conditions where safer alternatives are not effective.
Use with caution in patients with history of pancreatitis or total gastrectomy. Hepatic impairment requires caution. Electrolyte abnormalities such as hypokalaemia, hypomagnesaemia should be corrected before starting therapy. Adequate hydration should be maintained.
Symptoms may include neutropenia, vomiting, and drowsiness.
Management includes close monitoring and supportive care.
Targeted cancer therapy
Store in a cool (below 30°C), dry place, protected from light. Keep out of reach of children.
What is Nilotinib for?
What does Nilotinib do?
What are the side effects of Nilotinib?
What happens if you take too much Nilotinib?
Can Nilotinib be taken during pregnancy?
No available drugs found