Nilotinib Viatris (Nilotinib)

Nilotinib is employed in the management of chronic myeloid leukemia, targeting the BCR‑ABL tyrosine kinase pathway.

• Chronic myeloid leukemia – chronic phase: helps achieve cytogenetic and molecular remission, reducing disease burden.
• Chronic myeloid leukemia – accelerated phase: contributes to disease control and prolongs progression‑free survival.
• Chronic myeloid leukemia – blast phase: used as part of combination therapy to lower leukemic blast counts.
• Imatinib‑resistant or intolerant CML: provides an alternative targeted therapy for patients who cannot continue first‑line treatment.
• Post‑allogeneic stem cell transplant CML: may be used to prevent disease relapse in the maintenance setting.

• Nilotinib binds competitively to the ATP‑binding site of the BCR‑ABL fusion protein, inhibiting its tyrosine kinase activity. By blocking phosphorylation of downstream substrates, it suppresses signaling pathways that drive proliferation and survival of leukemic cells, including those harboring imatinib‑resistant mutations. The inhibition also affects related kinases such as KIT and PDGFR, contributing to its antineoplastic effect. The selective inhibition results in reduced tumor cell growth while sparing most normal cells.

Nilotinib may cause a range of adverse reactions, which are categorized by frequency and severity.

Common Side Effects

• Nausea: mild to moderate upset stomach often occurring early in therapy.
• Rash: skin eruptions that may be pruritic or non‑itchy.
• Fatigue: persistent tiredness not relieved by rest.
• Headache: mild to moderate head pain.

Serious or Rare Side Effects

• QT prolongation: cardiac electrical disturbance that can lead to arrhythmia.
• Pancreatitis: inflammation of the pancreas presenting with abdominal pain.
• Severe hepatic injury: marked elevation of liver enzymes and possible liver failure.

When prescribing nilotinib, clinicians should observe several precautionary measures to ensure patient safety.

• ECG monitoring: perform baseline and periodic ECGs to detect QT interval changes.
• Hepatic function: assess liver enzymes before initiation and during treatment.
• Infection risk: monitor for signs of infection, especially in immunocompromised patients.
• Cardiovascular disease: use caution in patients with existing heart conditions.
• Concomitant CYP3A4 inhibitors: avoid strong inhibitors that may increase drug exposure.
• Store at ambient temperature: keep tablets in the original container, protect from moisture and light.

Nilotinib interacts with several medicines; awareness of these interactions helps maintain therapeutic effectiveness and reduce toxicity.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors: agents such as ketoconazole markedly raise nilotinib plasma levels.
• QT‑prolonging drugs: co‑administration with other QT‑extending agents increases arrhythmia risk.
• Antacids containing aluminum/magnesium: reduce nilotinib absorption when taken simultaneously.

Moderate Interactions (Monitor Closely)

• CYP3A4 inducers: drugs like rifampin may lower nilotinib concentrations, reducing efficacy.
• H2 blockers or PPIs: agents such as cimetidine or omeprazole can affect nilotinib bioavailability.