Nilotinib Viatris (Nilotinib)

Nilotinib is indicated for diseases driven by the BCR‑ABL fusion protein, primarily chronic myeloid leukemia.

• Chronic myeloid leukemia (CML): Reduces disease progression and improves survival in adult patients with Philadelphia chromosome‑positive CML.
• Philadelphia chromosome‑positive acute lymphoblastic leukemia (Ph+ ALL): Used as part of combination therapy to achieve remission in selected adult patients.
• Imatinib‑resistant or intolerant CML: Provides an alternative therapeutic option when prior tyrosine kinase inhibitor therapy fails.

• Nilotinib selectively binds to the ATP‑binding site of the BCR‑ABL tyrosine kinase, inhibiting its catalytic activity. This blockade prevents phosphorylation of downstream signaling proteins, halting proliferation of malignant leukemic cells. The drug also inhibits related kinases such as c‑KIT and platelet‑derived growth factor receptors, contributing to its antineoplastic effect. By maintaining sustained inhibition, nilotinib achieves durable molecular responses in responsive patients.

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

Common Side Effects

• Nausea
• Diarrhea
• Rash

Serious or Rare Side Effects

• QT interval prolongation with risk of arrhythmia
• Hepatotoxicity (elevated liver enzymes)
• Severe neutropenia or thrombocytopenia

When prescribing nilotinib, clinicians should consider several safety precautions to minimize risk.

• Cardiac monitoring: Baseline and periodic ECGs are recommended to detect QT prolongation.
• Hepatic function: Assess liver enzymes before initiation and monitor during therapy.
• Pancreatic enzymes: Check amylase and lipase levels periodically.
• Pregnancy risk: Contraindicated in pregnancy (Category D); effective contraception is required.
• Drug interactions: Avoid concomitant use with strong CYP3A4 inhibitors or inducers.
• Store at ambient temperature below 25°C: Keep in the original container, protect from moisture and light.

Nilotinib interacts with several medicines that can alter its plasma concentration or increase toxicity.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): May raise nilotinib levels and risk cardiac toxicity.
• Strong CYP3A4 inducers (e.g., rifampin, phenytoin): May reduce efficacy by lowering drug exposure.
• Anti‑arrhythmic agents that prolong QT (e.g., amiodarone): Combined use can exacerbate QT prolongation.

Moderate Interactions (Monitor Closely)

• CYP3A4 substrate drugs (e.g., statins, calcium channel blockers): May require dose adjustment.
• Gastric pH modifiers (e.g., proton pump inhibitors, antacids): Can affect nilotinib absorption.
• Anticoagulants (e.g., warfarin): May increase bleeding risk; monitor INR closely.