Nilotinib Viatris (Nilotinib)

Nilotinib is a targeted tyrosine‑kinase inhibitor used in the management of Philadelphia chromosome‑positive chronic myeloid leukemia.

• Chronic phase CML: induces hematologic, cytogenetic and molecular remission.
• Accelerated phase CML: improves disease control in patients who have failed prior tyrosine‑kinase inhibitor therapy.
• Philadelphia‑positive CML after prior therapy: provides an alternative option for patients resistant or intolerant to imatinib.

• Nilotinib binds to the ATP‑binding site of the BCR‑ABL fusion protein, inhibiting its tyrosine‑kinase activity. By blocking downstream signaling pathways such as RAS‑MAPK, PI3K‑AKT, and STAT, the drug suppresses proliferation and induces apoptosis of leukemic cells, including many mutant forms of BCR‑ABL.

Common Side Effects

• Nausea: mild to moderate gastrointestinal upset.
• Diarrhea: loose stools, often transient.
• Rash: skin erythema or pruritus.
• Headache: mild to moderate intensity.
• Fatigue: generalized tiredness.
• Vomiting: occasional episodes.

Serious or Rare Side Effects

• QT interval prolongation: risk of cardiac arrhythmias.
• Pancreatitis: severe abdominal pain with elevated enzymes.
• Hepatotoxicity: significant elevation of liver transaminases.
• Severe neutropenia: marked reduction in white blood cells.
• Severe thrombocytopenia: low platelet counts leading to bleeding risk.
• Anaphylaxis: rare severe allergic reaction.

Nilotinib requires careful monitoring due to its safety profile.

• Cardiac monitoring: obtain baseline ECG and repeat periodically because of QT‑prolongation risk.
• Hepatic function: assess liver enzymes before initiation and during treatment.
• Hematologic surveillance: regular complete blood counts to detect myelosuppression.
• Concomitant QT‑prolonging drugs: avoid or use with caution to prevent arrhythmia.
• Pregnancy and lactation: contraindicated; discuss risks with a physician.
• Store at room temperature below 25°C: keep in the original packaging, protect from moisture and light.

Nilotinib has several clinically relevant drug interactions.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may increase nilotinib exposure and toxicity.
• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): may reduce efficacy by lowering plasma levels.
• Other QT‑prolonging agents (e.g., amiodarone, sotalol): increase risk of serious cardiac arrhythmias.

Moderate Interactions (Monitor Closely)

• Antacids containing aluminum or magnesium: can reduce nilotinib absorption; separate dosing by at least 2 hours.
• CYP3A4‑metabolized statins (e.g., simvastatin, lovastatin): may raise statin concentrations; consider dose adjustment.
• Warfarin: may require more frequent INR monitoring due to potential interaction.