Nilotinib
TASIGNA
Pronunciation: nye-LOE-ti-nib
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.
Nilotinib prescription history
Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Nilotinib enters in 2007 (estimated).
FDA-approved for
- CML (2007)
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Newly diagnosed Ph+ CML, chronic phase | Adults | 300 mg BID | 300 mg BID | 300 mg BID |
| Ph+ CML-CP/AP resistant or intolerant to prior imatinib | Adults | 400 mg BID | 400 mg BID | 400 mg BID |
| Newly diagnosed Ph+ CML, chronic phase | Pediatric ≥1 yr | 230 mg/m2 BID (rounded to nearest 50 mg) | 230 mg/m2 BID (rounded to nearest 50 mg) | 400 mg per dose (800 mg/day) |
| Ph+ CML-CP/AP resistant or intolerant to prior TKI | Pediatric ≥1 yr | 230 mg/m2 BID (rounded to nearest 50 mg) | 230 mg/m2 BID (rounded to nearest 50 mg) | 400 mg per dose (800 mg/day) |
Renal Undefined
Hepatic Newly diagnosed CML-CP, any Child-Pugh: 200 mg BID, ↑300 mg BID as tolerated. Resistant/intolerant: mild–moderate 300 mg BID (↑400 mg BID); severe 200 mg BID (↑300 then 400 mg BID). Monitor QT.
ECG at baseline, 7 days after start, and after dose changes. Unavoidable strong CYP3A4 inhibitor: 200 mg QD (newly diagnosed) or 300 mg QD (resistant/intolerant). Treatment-free remission may be considered after ≥3 years with sustained MR4.5.
Instructions
- BID ~12 h apart on empty stomach: no food ≥2 h before and ≥1 h after each dose
- Swallow capsules whole with water; if unable, disperse contents in 1 teaspoon applesauce and take within 15 minutes
- Correct hypokalemia/hypomagnesemia before starting
Available strengths
- cap 50, 150, 200 mg
- tab 71, 95 mg
- ODT 60, 80 mg
Contraindications
- Hypokalemia
- Hypomagnesemia
- Long QT syndrome
Cautions
- Myelosuppression
- QT prolongation
- Sudden deaths
- Cardiac and arterial vascular occlusive events
- Pancreatitis and elevated serum lipase
- Hepatotoxicity
- Electrolyte abnormalities
- Tumor lysis syndrome
- Hemorrhage
- Total gastrectomy
- Lactose content
- Monitoring laboratory tests
- Fluid retention
- Growth and development effects in pediatrics
- Embryo-fetal toxicity
- BCR-ABL monitoring after treatment discontinuation
Adverse reactions
- Nausea
- Rash
- Headache
- Fatigue
- Pruritus
- Vomiting
- Diarrhea
- Cough
- Constipation
- Arthralgia
- Nasopharyngitis, pyrexia, night sweats
- Myelosuppression (thrombocytopenia, neutropenia, anemia)
Pregnancy Can cause fetal harm (animal data and mechanism); no human data; advise effective contraception.
Lactation Present in rat milk; do not breastfeed during treatment and for 14 days after the last dose.
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 50 mg | cap | 60 BID | offered | |
| 150 mg | cap | 60 BID | offered | |
| 200 mg | cap | 60 BID | out of stock |
Generic entry2024
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Self-check
- How must nilotinib be taken relative to meals?
Fasting. - What cardiac monitoring is required with nilotinib?
ECG monitoring.