Nilotinib (TASIGNA)

Philadelphia chromosome positive (Ph+) Chronic myeloid leukemia

Philadelphia chromosome positive (Ph+) Chronic myeloid leukemia

• Oral: Chronic phase, newly diagnosed – 300mg twice daily continuously until disease progression or unacceptable toxicity  
• Oral: Resistant chronic phase, or accelerated or blast phase – 400mg twice daily  continuously until disease progression or unacceptable toxicity

Available as 150 mg and 200 mg capsules. Contains lactose. Capsules should NOT be opened. Store at room temperature.

BCR-ABL Tyrosine Kinase Inhibitor

Take on an empty stomach, at least 1 hour before or 2 hours after food

If a dose is missed, patients should be instructed not to take the missed dose but to resume with the next scheduled dose.

Common: Fatigue, Pruritus, Rash, Nausea, Diarrhea, Myalgia/arthralgia, Headache.

Less Common: Anemia, Neutropenia, Thrombocytopenia, Hyperglycemia, Amylase/lipase increased, Increase liver function tests.

The adverse effects listed above are not exhaustive. Please refer to the relevant product monograph for full details.

Baseline before treatment: CBC & differential, platelets, ALT, bilirubin, serum creatinine, BUN, lipase, GGT, body weight, bone marrow examination for cytogenetic analysis, FISH, RT-PCR (for BCR/ABL transcripts), BCR-ABL mutational analysis, ECG, HBsAg, HBcoreAb.

For disease progression:

• CBC & differential, platelets: weekly until complete hematological response, then monthly
  • after 6 months and if patient is clinically stable, may increase interval to every 3 months at the physician’s discretion
• Serum creatinine, uric acid, ALT, bilirubin: weekly until stable then monthly.
  • after 6 months and if patient is clinically stable, may increase interval to every 3 months at the physician’s discretion.
• BCR-ABL transcripts every 3 months until MMR achieved and maintained for at least 12 months.
  • Frequency of transcript testing can then move to every 6 months.

Monitoring for dose modifications:

• First month: Weekly CBC & differential, Platelets, ALT, Bilirubin, lipase, glucose.

• Month 2-6: Monthly CBC & differential, Platelets, ALT, Bilirubin, lipase, glucose.
• After 6 months: CBC & differential, Platelets, ALT, Bilirubin, lipase, glucose every 3 months.

ECG should be repeated 1 week after initially starting Nilotinib, and 1 week after any dose change.

• May increase the risk for QT interval prolongation. Avoid concurrent therapy with drugs associated with QTc prolongation and/or Torsades de pointes, if possible. If unavoidable, monitor for QT prolongation or cardiac arrhythmias.
• This drug can impact or be impacted by metabolic enzymes for absorption and excretion. Many drugs can also affect or be affected by these enzymes, so please consult with pharmacy to assess for interactions.
• Avoid grapefruit, grapefruit juice, Seville oranges, or Seville orange juice.
• Current drug interaction databases should be consulted for more information.

• Avoid in pregnancy and lactation.
• Reactivation of hepatitis B virus (HBV) has been reported in patients who are chronic carriers of HBV and received BCR-ABL TKIs. Patients should be tested for HBV infection prior to initiating treatment. Carriers of HBV must be monitored for signs and symptoms of active HBV infection throughout therapy and for several months following termination of therapy.

BC Cancer. BC Cancer Drug Manual. Nilotinib.  Vancouver, British Columbia: BC Cancer Agency. Available at: http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Nilotinib_monograph.pdf. Updated February 1, 2024. Accessed February 14, 2024.

Lexicomp. Nilotinib Monograph. In: Lexi-Drugs. Hudson, Ohio: Lexi-Comp, Inc. Available at: https://online-lexi-com.qe2a-proxy.mun.ca/lco/action/doc/retrieve/docid/patch_f/1020618?cesid=2xg03cAVQot&searchUrl=%2Flco%2Faction%2Fsearch%3Fq%3Dnilotinib%26t%3Dname%26acs%3Dfalse%26acq%3Dnilotinib. Updated January 24, 2024. Accessed January 31, 2024.

Cancer Care Ontario. Nilotinib Monograph. Drug Formulary. Toronto, Ontario: Cancer Care Ontario. Available at: https://www.cancercareontario.ca/en/drugformulary/drugs/monograph/43941. Updated December 2023. Accessed January 22, 2024.

Novartis Pharmaceuticals Canada Inc. TASIGNA® Product monograph. Dorval, Quebec. Updated August 19, 2015.