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Tasigna

nilotinib
BCR-ABL Tyrosine Kinase Inhibitor Novartis FDA Approved 2007
Indications Dosing Forms Contraindications Warnings Adverse Reactions Pharmacology Clinical Studies Tumor Types
1. Indications and Usage

Newly diagnosed adult patients with Ph+ CML in chronic phase; Ph+ CML in chronic or accelerated phase resistant to or intolerant of prior therapy including imatinib; Pediatric Ph+ CML in chronic phase.

2. Dosage and Administration

Newly diagnosed CML-CP: 300 mg orally twice daily
Resistant/intolerant CML: 400 mg orally twice daily
MUST be taken on empty stomach — no food 2 hours before and 1 hour after dose
QTc monitoring: ECG at baseline, 7 days after initiation, periodically, and after dose adjustments

3. Dosage Forms and Strengths

Capsules: 50 mg, 150 mg, 200 mg

4. Contraindications

Hypokalemia, hypomagnesemia, or long QT syndrome.

5. Warnings and Precautions
⚠ Boxed Warning
QT PROLONGATION AND SUDDEN DEATHS: Nilotinib prolongs the QT interval. Sudden deaths have been reported. Do not administer to patients with hypokalemia, hypomagnesemia, or long QT syndrome. Correct electrolytes prior to and during administration. Monitor ECGs.
  • QT Prolongation: Sudden deaths in 0.3%. Monitor ECGs and electrolytes. Avoid drugs that prolong QT.
  • Myelosuppression: Grade 3-4 neutropenia (31%), thrombocytopenia (29%), anemia (10%). Monitor CBC every 2 weeks × 2 months, then monthly.
  • Cardiovascular Events: Peripheral arterial occlusive disease (PAOD), ischemic heart disease, and ischemic cerebrovascular events in 2-10%. Monitor for signs of vascular events.
  • Pancreatitis: Grade 3-4 in 2%. Monitor lipase monthly or as needed.
  • Hepatotoxicity: Grade 3-4 bilirubin elevations in 4%, transaminases in 4%. Monitor LFTs monthly.
  • Tumor Lysis Syndrome
6. Adverse Reactions
Most Common Adverse Reactions

Rash (36%), headache (32%), nausea (31%), fatigue (28%), pruritus (26%), myalgia (19%), upper abdominal pain (18%), constipation (16%), diarrhea (15%), vomiting (15%), alopecia (13%), arthralgia (12%)

Rash
36%
Headache
32%
Nausea
31%
Fatigue
28%
Pruritus
26%
Myalgia
19%
Upper Abdominal Pain
18%
Constipation
16%
Diarrhea
15%
Vomiting
15%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

12. Clinical Pharmacology
Mechanism of Action

Nilotinib is a BCR-ABL kinase inhibitor designed to overcome imatinib resistance. It binds to the inactive conformation of the ABL kinase domain with approximately 20-fold higher potency than imatinib. Nilotinib also inhibits PDGFR, c-KIT, and DDR kinases. It is active against 32 of 33 imatinib-resistant BCR-ABL mutations (not T315I).

Pharmacokinetics

Tmax: 3 hours. Half-life: approximately 17 hours. Protein binding: ~98%. Metabolized by CYP3A4 and CYP2C8. Bioavailability increased ~82% with food (must be fasted). Steady-state by Day 8. Excreted primarily in feces (93%).

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
📋 All Nilotinib Trials on ClinicalTrials.gov ↗ 📚 PubMed: Nilotinib Clinical Trials ↗
Approved Tumor Types
Chronic Myeloid Leukemia