Nilotinib
TASIGNA
What it isSecond-generation BCR-ABL inhibitor; chronic myeloid leukemia.
Why this oneDeeper molecular responses than imatinib, which supports attempting treatment-free remission.
What limits itQT prolongation and sudden death, so it must be taken fasting and ECG monitored. Vascular occlusive events; hyperglycemia.
FDA-approved for
- CML (2007)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Newly diagnosed Ph+ CML in chronic phase | adult | 120 mg BID | 120 mg BID | 120 mg BID |
| Resistant or intolerant Ph+ CML-CP and CML-AP | adult | 160 mg BID | 160 mg BID | 160 mg BID |
Renal Undefined
Hepatic Reduce starting dose in hepatic impairment and monitor QT closely
Instructions
- Take twice daily about 12 hours apart, with or without food
- Use dry hands; place tablet on the tongue to disintegrate, then swallow with saliva; may chew or swallow whole with water; do not crush
- Not substitutable mg-per-mg with other nilotinib products (e.g., Tasigna) — use the conversion
- Correct hypokalemia/hypomagnesemia before starting
Contraindications
- Hypokalemia
- Hypomagnesemia
- Long QT syndrome
Cautions
- Myelosuppression
- QT prolongation and sudden death
- Cardiac and arterial vascular occlusive events
- Pancreatitis and elevated lipase
- Hepatotoxicity
- Electrolyte abnormalities
- Tumor lysis syndrome
- Hemorrhage
- Fluid retention
- Embryo-fetal toxicity
Adverse reactions
- Nausea
- Rash
- Headache
- Fatigue
- Pruritus
- Vomiting
- Diarrhea
- Thrombocytopenia
- Neutropenia
- Anemia
Pregnancy Can cause fetal harm (animal data); advise effective contraception
Lactation Do not breastfeed during treatment and for 14 days after the last dose
⚠ BOXED WARNING
- QT prolongation and sudden death
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2024
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Nilotinib ballicule
