1 yr who are resistant or intolerant to prior tyrosine-kinase inhibitor treatment.Contraindicated in:
Use Cautiously in:
CV: hypertension, MI, palpitations, pericardial effusion, peripheral arterial disease, QT interval prolongation, TORSADES DE POINTES.
Derm: pruritus, rash, alopecia, flushing.
EENT: vertigo.
F and E: hyperkalemia, hypocalcemia, hypokalemia, hyponatremia, hypophosphatemia.
GI: ↑lipase, constipation, diarrhea, nausea, vomiting, abdominal discomfort, anorexia, ascites, dyspepsia, flatulence, hepatitis B virus reactivation, HEPATOTOXICITY.
Hemat: bleeding, myelosupression.
Metab: hyperglycemia.
MS: ↓growth, musculoskeletal pain.
Neuro: fatigue, headache, dizziness, paresthesia, STROKE.
Resp: pleural effusion, pulmonary edema.
Misc: fever, night sweats, tumor lysis syndrome.
Drug-Drug:
Drug-Natural Products:
Drug-Food:
Newly Diagnosed Chronic Phase Ph+ Chronic Myelogenous Leukemia
3 yr and achieved a sustained molecular response; if patients lose molecular response after discontinuing therapy, restart nilotinib within 4 wk at the dose level prior to discontinuation. Concurrent use of strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, or voriconazole): 200 mg once daily.1 yr): 230 mg/m2 twice daily (max single dose = 400 mg) until disease progression or unacceptable toxicity; treatment discontinuation may be considered in patients who have received nilotinib for 3 yr and achieved a sustained molecular response; if patients lose molecular response after discontinuing therapy, restart nilotinib within 4 wk at the dose level prior to discontinuation. Concurrent use of strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, or voriconazole): 200 mg once daily.Hepatic Impairment
1 yr): Mild, moderate, or severe hepatic impairment: 200 mg twice daily; may ↑ to 300 mg twice daily if tolerates.Resistant or Intolerant Chronic or Accelerated Phase Ph+ Chronic Myelogenous Leukemia
3 yr and achieved a sustained molecular response; if patients lose molecular response after discontinuing therapy, restart nilotinib within 4 wk at the dose level prior to discontinuation. Concurrent use of strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, or voriconazole): 300 mg once daily.1 yr): 230 mg/m2 twice daily (max single dose = 400 mg) until disease progression or unacceptable toxicity; treatment discontinuation may be considered in patients who have received nilotinib for 3 yr and achieved a sustained molecular response; if patients lose molecular response after discontinuing therapy, restart nilotinib within 4 wk at the dose level prior to discontinuation. Concurrent use of strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, or voriconazole): 200 mg once daily.Hepatic Impairment
1 yr): Mild or moderate hepatic impairment: 300 mg twice daily; may ↑ to 400 mg twice daily if tolerated. Severe hepatic impairment: 200 mg twice daily; may ↑ to 300 mg twice daily, and eventually to 400 mg twice daily if tolerated.Therapeutic Classification: antineoplastics
Pharmacologic Classification: enzyme inhibitors, kinase inhibitors
Absorption: Well absorbed following oral administration. Levels are significantly ↑ by food.
Distribution: Unknown.
Metabolism/Excretion: Mostly metabolized by the liver via the CYP3A4 isoenzyme to inactive metabolites. Primarily excreted in the feces (93%), with 69% being excreted unchanged.
Half-life: 17 hr.
14 days following last dose and to avoid breastfeeding for 14 days following last dose. Advise patient to notify health care professional immediately if pregnancy is suspected.NDC Code*