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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › BCR-ABL tyrosine kinase inhibitors
nilotinib
L01EA03
Forms & Strengths
- Capsules: 50 mg
- Capsules: 150 mg
- Capsules: 200 mg
Adult Dosing
- Newly diagnosed Ph+ CML-CP: 300 mg orally twice daily
- Resistant/intolerant Ph+ CML-CP and CML-AP: 400 mg orally twice daily
- Take on an empty stomach (no food 2 hours before and 1 hour after dose)
Pediatric Dosing
- Pediatric patients 1 year of age and older with newly diagnosed Ph+ CML-CP: 230 mg/m2 orally twice daily (rounded to nearest 50 mg dose, max single dose 400 mg)
- Pediatric patients with resistant/intolerant Ph+ CML-CP and CML-AP: 230 mg/m2 orally twice daily
Indications
- Treatment of newly diagnosed Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase
- Treatment of chronic phase and accelerated phase Ph+ CML resistant or intolerant to prior therapy including imatinib
Mechanism of Action
- Tyrosine kinase inhibitor that targets Bcr-Abl, KIT, PDGFR, and ephrin receptor kinases
- Potently inhibits the Bcr-Abl oncoprotein, inducing apoptosis in cell lines and primary CML cells expressing mutant and wild-type forms of Bcr-Abl
Contraindications
- Hypokalemia or hypomagnesemia (must be corrected prior to administration)
- Long QT syndrome
Adverse Reactions
- Myelosuppression (thrombocytopenia, neutropenia, anemia)
- QTc prolongation and sudden death
- Cardiovascular events (ischemic heart disease, peripheral arterial occlusive disease, ischemic cerebrovascular events)
- Hepatotoxicity (elevated transaminases and bilirubin)
- Pancreatitis and elevated serum lipase
- Rash, pruritus, headache, fatigue, nausea, constipation, diarrhea
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, ritonavir) increase nilotinib exposure and risk of toxicity; avoid concurrent use
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort) decrease nilotinib exposure; avoid concurrent use
- Drugs that prolong the QT interval (e.g., antiarrhythmics) increase the risk of torsades de pointes; avoid concurrent use
- Drugs that elevate gastric pH (e.g., proton pump inhibitors, H2 blockers, antacids) may decrease nilotinib bioavailability; separate administration times
Curated Content: Needs Vetting Before Put to Clinical Use